Benzylidene Compounds: Compounds containing the PhCH= radical.PiperidonesAnabasine: A piperidine botanical insecticide.AcetalsEchinochloa: A plant genus of the family POACEAE that is grown mainly as a hay crop.Molecular Structure: The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.Drug Screening Assays, Antitumor: Methods of investigating the effectiveness of anticancer cytotoxic drugs and biologic inhibitors. These include in vitro cell-kill models and cytostatic dye exclusion tests as well as in vivo measurement of tumor growth parameters in laboratory animals.Structure-Activity Relationship: The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.Awards and PrizesMetabolomics: The systematic identification and quantitation of all the metabolic products of a cell, tissue, organ, or organism under varying conditions. The METABOLOME of a cell or organism is a dynamic collection of metabolites which represent its net response to current conditions.Canada: The largest country in North America, comprising 10 provinces and three territories. Its capital is Ottawa.Alberta: A province of western Canada, lying between the provinces of British Columbia and Saskatchewan. Its capital is Edmonton. It was named in honor of Princess Louise Caroline Alberta, the fourth daughter of Queen Victoria. (From Webster's New Geographical Dictionary, 1988, p26 & Room, Brewer's Dictionary of Names, 1992, p12)British Columbia: A province of Canada on the Pacific coast. Its capital is Victoria. The name given in 1858 derives from the Columbia River which was named by the American captain Robert Gray for his ship Columbia which in turn was named for Columbus. (From Webster's New Geographical Dictionary, 1988, p178 & Room, Brewer's Dictionary of Names, 1992, p81-2)Sodium Benzoate: The sodium salt of BENZOIC ACID. It is used as an antifungal preservative in pharmaceutical preparations and foods. It may also be used as a test for liver function.Polypropylenes: Propylene or propene polymers. Thermoplastics that can be extruded into fibers, films or solid forms. They are used as a copolymer in plastics, especially polyethylene. The fibers are used for fabrics, filters and surgical sutures.Benzoic Acid: A fungistatic compound that is widely used as a food preservative. It is conjugated to GLYCINE in the liver and excreted as hippuric acid.Benzoates: Derivatives of BENZOIC ACID. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain the carboxybenzene structure.Cinnamomum zeylanicum: The tree which is known for its bark which is sold as cinnamon. The oil contains about 65-80% cinnamaldehyde and 10% EUGENOL and many TERPENES.Food Preservatives: Substances capable of inhibiting, retarding or arresting the process of fermentation, acidification or other deterioration of foods.Guaifenesin: An expectorant that also has some muscle relaxing action. It is used in many cough preparations.4-Aminobenzoic Acid: An aminobenzoic acid isomer that combines with pteridine and GLUTAMIC ACID to form FOLIC ACID. The fact that 4-aminobenzoic acid absorbs light throughout the UVB range has also resulted in its use as an ingredient in SUNSCREENS.HEPES: A dipolar ionic buffer.meta-Aminobenzoates: Aminobenzoate derivatives that contain an amino group attached to carbon number 3 or 5 of the benzene ring structure.Magnesium Sulfate: A small colorless crystal used as an anticonvulsant, a cathartic, and an electrolyte replenisher in the treatment of pre-eclampsia and eclampsia. It causes direct inhibition of action potentials in myometrial muscle cells. Excitation and contraction are uncoupled, which decreases the frequency and force of contractions. (From AMA Drug Evaluations Annual, 1992, p1083)Sodium Bicarbonate: A white, crystalline powder that is commonly used as a pH buffering agent, an electrolyte replenisher, systemic alkalizer and in topical cleansing solutions.ortho-Aminobenzoates: Benzoic acids, salts, or esters that contain an amino group attached to carbon number 2 or 6 of the benzene ring structure.Aminobenzoates: Derivatives of BENZOIC ACID that contain one or more amino groups attached to the benzene ring structure. Included under this heading are a broad variety of acid forms, salts, esters, and amides that include the aminobenzoate structure.Gift Giving: The bestowing of tangible or intangible benefits, voluntarily and usually without expectation of anything in return. However, gift giving may be motivated by feelings of ALTRUISM or gratitude, by a sense of obligation, or by the hope of receiving something in return.Pancreatic Ducts: Ducts that collect PANCREATIC JUICE from the PANCREAS and supply it to the DUODENUM.BostonCarcinoma, Pancreatic Ductal: Carcinoma that arises from the PANCREATIC DUCTS. It accounts for the majority of cancers derived from the PANCREAS.Apoptosis: One of the mechanisms by which CELL DEATH occurs (compare with NECROSIS and AUTOPHAGOCYTOSIS). Apoptosis is the mechanism responsible for the physiological deletion of cells and appears to be intrinsically programmed. It is characterized by distinctive morphologic changes in the nucleus and cytoplasm, chromatin cleavage at regularly spaced sites, and the endonucleolytic cleavage of genomic DNA; (DNA FRAGMENTATION); at internucleosomal sites. This mode of cell death serves as a balance to mitosis in regulating the size of animal tissues and in mediating pathologic processes associated with tumor growth.Reagent Kits, Diagnostic: Commercially prepared reagent sets, with accessory devices, containing all of the major components and literature necessary to perform one or more designated diagnostic tests or procedures. They may be for laboratory or personal use.Pancreatic Neoplasms: Tumors or cancer of the PANCREAS. Depending on the types of ISLET CELLS present in the tumors, various hormones can be secreted: GLUCAGON from PANCREATIC ALPHA CELLS; INSULIN from PANCREATIC BETA CELLS; and SOMATOSTATIN from the SOMATOSTATIN-SECRETING CELLS. Most are malignant except the insulin-producing tumors (INSULINOMA).Patents as Topic: Exclusive legal rights or privileges applied to inventions, plants, etc.Metals: Electropositive chemical elements characterized by ductility, malleability, luster, and conductance of heat and electricity. They can replace the hydrogen of an acid and form bases with hydroxyl radicals. (Grant & Hackh's Chemical Dictionary, 5th ed)Salts: Substances produced from the reaction between acids and bases; compounds consisting of a metal (positive) and nonmetal (negative) radical. (Grant & Hackh's Chemical Dictionary, 5th ed)Inventions: A novel composition, device, or process, independently conceived de novo or derived from a pre-existing model.Intellectual Property: Property, such as patents, trademarks, and copyright, that results from creative effort. The Patent and Copyright Clause (Art. 1, Sec. 8, cl. 8) of the United States Constitution provides for promoting the progress of science and useful arts by securing for limited times to authors and inventors, the exclusive right to their respective writings and discoveries. (From Black's Law Dictionary, 5th ed, p1014)Foramen Ovale, Patent: A condition in which the FORAMEN OVALE in the ATRIAL SEPTUM fails to close shortly after birth. This results in abnormal communications between the two upper chambers of the heart. An isolated patent ovale foramen without other structural heart defects is usually of no hemodynamic significance.Nickel: A trace element with the atomic symbol Ni, atomic number 28, and atomic weight 58.69. It is a cofactor of the enzyme UREASE.Piperidines: A family of hexahydropyridines.p-Dimethylaminoazobenzene: A reagent used mainly to induce experimental liver cancer. According to the Fourth Annual Report on Carcinogens (NTP 85-002, p. 89) published in 1985, this compound "may reasonably be anticipated to be a carcinogen." (Merck, 11th ed)p-Aminoazobenzene: Used in the form of its salts as a dye and as an intermediate in manufacture of Acid Yellow, diazo dyes, and indulines.Methyldimethylaminoazobenzene: A very potent liver carcinogen.Hydroxyethyl Starch Derivatives: Starches that have been chemically modified so that a percentage of OH groups are substituted with 2-hydroxyethyl ether groups.Oxygen Inhalation Therapy: Inhalation of oxygen aimed at restoring toward normal any pathophysiologic alterations of gas exchange in the cardiopulmonary system, as by the use of a respirator, nasal catheter, tent, chamber, or mask. (From Dorland, 27th ed & Stedman, 25th ed)PyrrolidinesJapanHypertension: Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.Societies, Medical: Societies whose membership is limited to physicians.Genes, araC: Regulatory genes which encode a cyclic AMP receptor protein required for L-arabinose utilization in E. coli. It is an example of positive control or regulation of gene expression in the bacterial operon.Heat-Shock Proteins: Proteins which are synthesized in eukaryotic organisms and bacteria in response to hyperthermia and other environmental stresses. They increase thermal tolerance and perform functions essential to cell survival under these conditions.Organoselenium Compounds: Organic compounds which contain selenium as an integral part of the molecule.HSP70 Heat-Shock Proteins: A class of MOLECULAR CHAPERONES found in both prokaryotes and in several compartments of eukaryotic cells. These proteins can interact with polypeptides during a variety of assembly processes in such a way as to prevent the formation of nonfunctional structures.

Sugars and sugar derivatives which inhibit the short-circuit current of the everted small intestine of the rat. (1/210)

1. The short-circuit current of everted rat intestine supported on a perforated cannula proved to be stable for up to 3 hr and has been used to study competition between transportable and non-transportable sugars. 2. 4,6-O-Ethylidene-alpha-D-glucopyranose (ethylidene glucose) and 4,6-O-benzylidene-e alpha-D-glucopyranos (benzylinene glucose), two nontransportable inhibitors of the hexose transfer system in human erythrocytes, were found to reduce the short-circuit current generated by transportable sugars such as galactose or 3-O-methyl glucose. 3. These compounds were also found to reduce the basal short-circuit current established by the everted intestine in a sugar-free Krebs solution. Both types of inhibition approached saturation at the higher concentrations used. 4. Similar inhibitory properties were shown by mannose, a non-actively accumulated monosaccharide, and by the beta-disaccharides lactose and cellobiose. 5. It is suggested that this common pattern of behaviour is due to the ability of these compounds to react with the sites for active hexose transfer but without translocation by the system. The significance of the inhibition of the basal short-circuit current is briefly discussed in this context.  (+info)

Opioid-induced second window of cardioprotection: potential role of mitochondrial KATP channels. (2/210)

Opioids have been previously shown to confer short-term cardioprotection against a prolonged ischemic insult. Therefore, the present study was designed to determine whether opioids can induce a delayed or "second window" of cardioprotection and to assess the potential involvement of the mitochondrial KATP channel. All rats were subjected to 30 minutes of ischemia and 2 hours of reperfusion (I/R). Control animals, injected with saline 24 hours before I/R, elicited an infarct size/area at risk (IS/AAR) of 62.9+/-3.4. TAN-67, a delta1-opioid receptor agonist, was administered 10 or 30 mg/kg IP 12, 24, 48, or 72 hours before I/R. TAN-67 (10 mg/kg) 12- or 24-hour pretreatment did not significantly reduce IS/AAR (62.1+/-6.3 and 43.3+/-7.3, respectively). Similarly, 12-hour pretreatment with TAN-67 (30 mg/kg) did not reduce IS/AAR (60.0+/-5.6); however, 24-hour pretreatment significantly reduced IS/AAR (34.5+/-5.9). Forty-eight-hour pretreatment with TAN-67 maximally reduced IS/AAR (29.2+/-7.0), and opioid-induced cardioprotection was lost after 72-hour pretreatment (61.7+/-3.8). TAN-67-induced cardioprotection could be abolished by pretreatment with the selective delta1-opioid receptor antagonist 7-benzylidenenaltrexone, BNTX, administered either 30 minutes before TAN-67 given 48 hours before I/R or 10 minutes before I/R in rats previously treated for 48 hours with TAN-67 (59.6+/-3.1 and 58.7+/-3.5, respectively). The involvement of the KATP channel was investigated with 2 inhibitors: glibenclamide, a nonselective KATP channel inhibitor, and 5-hydroxydecanoic acid, selective for the mitochondrial KATP channel in rabbits. Glibenclamide, administered 30 minutes before I/R in 48-hour TAN-67-pretreated rats, completely abolished cardioprotection (60. 4+/-3.2). Similarly, 5-hydroxydecanoic acid, administered 5 minutes before I/R in rats pretreated 48 hours previously with TAN-67, completely abolished cardioprotection (57.8+/-2.5). These results suggest that delta1-opioid receptor stimulation, 24 to 48 hours before an ischemic insult, produces a delayed cardioprotective effect that is possibly the result of mitochondrial KATP channel activation.  (+info)

In vivo efficacy of XR9051, a potent modulator of P-glycoprotein mediated multidrug resistance. (3/210)

Overexpression of P-glycoprotein (P-gp) is a potential cause of multidrug resistance (MDR) in tumours. We have previously reported that XR9051 (N-(4-(2-(6,7-dimethoxy-1,2,3,4-tetrahydro-2-isoquinolyl)ethyl)phe nyl)-3-((3Z,6Z)-6-benzylidene-1-methyl-2,5-dioxo-3-pipera zinylidene)methylbenzamide) is a potent and specific inhibitor of P-gp, which reverses drug resistance in several murine and human MDR cell lines. In this study we have evaluated the in vivo efficacy of this novel modulator in a panel of murine and human tumour models and examined its pharmacokinetic profile. Efficacy studies in mice bearing MDR syngeneic tumours (P388/DX Johnson, MC26) or human tumour xenografts (A2780AD, CH1/DOXr, H69/LX) demonstrated that co-administration of XR9051 significantly potentiated the anti-tumour activity of a range of cytotoxic drugs. This modulatory activity was observed following parenteral and oral co-administration of XR9051. In addition, the combination schedules were well-tolerated. Following intravenous administration in mice, XR9051 is rapidly distributed and accumulates in tumours and other tissues. In addition, the compound is well-absorbed after oral administration. These data suggest that XR9051 has the potential for reversing clinical MDR mediated by P-glycoprotien.  (+info)

Effects of nicotinic receptor agonists on beta-amyloid beta-sheet formation. (4/210)

Previously we demonstrated that nicotinic acetylcholine receptor stimulation protects neurons against beta-amyloid (Abeta)-induced cytotoxicity. In the present study, the effects of nicotinic receptor agonists on the beta-sheet formation were investigated using a thioflavin T (ThT)-based fluorescence assay. Nicotine, cytisine (an alpha4beta2 agonist), and 3-(2,4)-dimethoxybenzylidene anabaseine (DMXB, an alpha7 agonist) did not reduce fluorescence intensity when these agents were added to the beta-sheet-formed Abeta. Simultaneous incubation of Abeta with nicotinic agonists also did not cause a reduction in fluorescence intensity. This data suggests that nicotinic receptor agonists do not influence the formation of the beta-sheet structure.  (+info)

In vivo effects of new inhibitors of catechol-O-methyl transferase. (5/210)

1. The effects of two new synthetic compounds showing in vitro catechol-O-methyl transferase (COMT) inhibitor properties were studied in vivo and compared with the effects of nitecapone and Ro-41-0960. 2. QO IA (3-(3-hydroxy-4-methoxy-5-nitrobenzylidene)-2,4-pentanedione), QO IIR ([2-(3,4-dihydroxy-2-nitrophenyl)vinyl]phenyl ketone), nitecapone and Ro-41-0960 (30 mg kg(-1), i.p.) were given to reserpinized rats 1 h before the administration of L-DOPA/carbidopa (LD/CD, 50:50 mg kg(-1), i.p.). Locomotor activity was assessed 1 h later. All the COMT inhibitors (COMTI), with the exception of QO IA, markedly potentiated LD/CD reversal of reserpine-induced akinesia. Similar results were obtained when the COMTI were coadministered with LD/CD. The effect of compound QO IIR was dose-dependent (7.5-30 mg kg(-1), i.p.). 3. The COMTI (30 mg kg(-1), i.p.) potentiated LD/CD reversal of both catalepsy and hypothermia of reserpinized mice. 4. QO IIR, nitecapone and Ro-41-0960 (30 mg kg(-1), i.p.) reduced striatal 3-methyl-DOPA (3-OMD) levels and increased dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) levels. Compound QO IA was devoid of any effect on striatal amine levels. In contrast to the other inhibitors, Ro-41-0961 reduced HVA levels as well. The effect of QO IIR on striatal amine levels was dose-dependent (7.5-60 mg kg(-1), i.p.) 5. These results suggest that the new compound QO IIR is an effective peripherally acting COMT inhibitor in vivo.  (+info)

Direct preconditioning of cardiac myocytes via opioid receptors and KATP channels. (6/210)

Previous studies demonstrated that opioid receptor activation mimics the cardioprotective effect of ischemic preconditioning via KATP channels in the intact heart. However, it is unknown whether this beneficial effect is exerted at the level of the cardiac myocyte or coronary vasculature or is mediated via the sarcolemmal or the mitochondrial KATP channel. Thus, the purpose of the present study was to investigate whether opioid receptor stimulation could mimic the cardioprotective effect of preconditioning in a cardiac myocyte model of simulated ischemia. Cardiac ventricular myocytes cultured from chick embryos 14 days in ovo were used as an in vitro model for ischemic preconditioning. A 5-minute exposure of the myocytes to the opioid receptor agonist morphine protected the myocytes during a subsequent 90-minute period of simulated ischemia, which was manifested as a pronounced reduction in the percentage of cardiac cells killed and the amount of creatine kinase released during ischemia. The preconditioning-like effect of morphine was concentration-dependent, reached a maximal effect at 1 micromol/L, and was reversed by naloxone (0.1 to 10 micromol/L). When KATP channel antagonists, such as glibenclamide, or the mitochondrial selective inhibitor 5-hydroxydecanoic acid were present during preexposure to morphine, they abolished the protective effect of morphine. Thus, cardiac myocytes express functional opioid receptors, and their activation mimics the cardioprotective effect of ischemic preconditioning. These results provide direct evidence that the preconditioning-like effect of morphine in the intact heart can be exerted at the level of cardiac myocytes and is most likely the result of mitochondrial KATP channel activation.  (+info)

Communication between multiple drug binding sites on P-glycoprotein. (7/210)

P-glycoprotein, a member of the ATP-binding cassette transporter family, is able to confer resistance on tumors against a large number of functionally and chemically distinct cytotoxic compounds. Several recent investigations suggest that P-glycoprotein contains multiple drug binding sites rather than a single site of broad substrate specificity. In the present study, radioligand-binding techniques were used to directly characterize drug interaction sites on P-glycoprotein and how these multiple sites interact. The drugs used were classified as either 1) substrates, which are known to be transported by P-glycoprotein (e.g., vinblastine) or 2) modulators, which alter P-glycoprotein function but are not themselves transported by the protein (e.g., XR9576). Drug interactions with P-glycoprotein were either competitive, at a common site, or noncompetitive, and therefore at distinct sites. Based on these data, we can assign a minimum of four drug binding sites on P-glycoprotein. These sites fall into two categories: transport, at which translocation of drug across the membrane can occur, and regulatory sites, which modify P-glycoprotein function. Intriguingly, however, some modulators interact with P-glycoprotein at a transport site rather than a regulatory site. The pharmacological data also demonstrate that both transport and regulatory sites are able to switch between high- and low-affinity conformations. The multiple sites on P-glycoprotein display complex allosteric interactions through which interaction of drug at one site switches other sites between high- or low-affinity conformations. The data are discussed in terms of a model for the mechanism of transport by P-glycoprotein.  (+info)

Transport of sugars and amino acids in bacteria. XV. Comparative studies on the effects of various energy poisons on the oxidative and phosphorylating activities and energy coupling reactions for the active transport systems for amino acids in E. coli. (8/210)

The effects of various energy poisons on oxidation of respiratory substrate, synthesis of cellular ATP, and energy transformation reaction in intact Escherichia coli cells were studied systematically. Various mutants were, therefore, used in which specific functions in the energy-transducing reactions were defective or altered. The energy poisons examined were: sodium azide. DPPA and azidebenzenes which are inhibitors of respiratory-chain phosphorylation, SF6847, and CCCP which are known to be uncouplers, zinc sulfate which is an inhibitor for certain dehydrogenases, and sodium arsenate and sodium fluoride which are inhibitors of glycolytic synthesis of ATP. The preferential inhibitions occurred in the oxidation reactions with certain respiratory substrates by energy poisons used. DPPA inhibited glycerol oxidation much more strongly than succinate oxidation. However, DPPA could inhibit the oxidation of both glycerol 3-phosphate and succinate by membrane fraction strongly while the oxidation of NADH and D-lactate slightly. It inhibited glycerol 3-phosphate dehydrogenase [EC 1.1.2.1] strongly as well as succinate dehydrogenase [EC 1.3.99.1],.but not D-lactate dehydrogenase of membrane fraction. MAB and other azidebenzene derivatives inhibited succinate oxidation preferentially. SF6847 and CCCP inhibited succinate oxidation strongly, while sodium azide inhibited it weakly and these three poisons were less inhibitory for glycerol oxidation. DPPA, sodium azide, SF6847, and CCCP inhibited the synthesis of ATP coupled with respiration but not with glycolysis. Zinc sulfate inhibited the cellular ATP synthesis coupled with either respiration or glycolysis.  (+info)

Stilbene Benzylidene compounds are alkene derivatives of benzene . They are primarily divided into two groups: Styrenes (one benzene ) Stilbenes (two benzenes ) Benzylidene is also used to describe a type of protecting group in synthetic organic chemistry of the form PhCH(R) For example, 4,6-O-benzylidene-glucopyranose is a glucose molecule whose 4- and 6-OH groups are protected by being bound to a benzylic carbon, forming a benzyl acetal. See also Dibenzylideneacetone Aurone External links Look up benzylidene in Wiktionary, the free dictionary. Benzylidene Compounds at the US National Library of Medicine Medical Subject Headings (MeSH) Stilbene Benzylidene compounds are alkene derivatives of benzene . They are primarily divided into two groups: Styrenes (one benzene ) Stilbenes (two benzenes ) Benzylidene is also used to describe a type of protecting group in synthetic organic chemistry of the form PhCH(R) For example, 4,6-O-benzylidene-glucopyranose is a glucose molecule whose 4- and 6-OH groups are
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Methods and Results-Studies were performed in vitro on cultured human smooth muscle cells, ex vivo on human arterial segments, and in vivo in a model consisting of human arterial segments grafted into severe combined immunodeficiency/beige mice injected weekly with anti-HLA antibodies. We report that anti-HLA antibodies are mitogenic for smooth muscle cells through a signaling mechanism implicating matrix metalloproteinases (MMPs) (membrane type 1 MMP and MMP2) and neutral sphingomyelinase-2. This mitogenic signaling and subsequent DNA synthesis are blocked in smooth muscle cells silenced for MMP2 or for neutral sphingomyelinase-2 by small interfering RNAs, in smooth muscle cells transfected with a vector coding for a dominant-negative form of membrane type 1 MMP, and after treatment by pharmacological inhibitors of MMPs (Ro28-2653) or neutral sphingomyelinase-2 (GW4869). In vivo, Ro28-2653 and GW4869 reduced the intimal thickening induced by anti-HLA antibodies in human mesenteric arteries ...
2,3-Di-O-benzyl-4,6-O-benzylidene-thiohexopyranosides, on activation with 1-benzenesulfinyl piperidine and triflic anhydride, react with allyl silanes and stannanes, and with silyl enolethers to give C-glycosides. In the mannose series the beta-isomers are formed selectively whereas the glucose series provides the alpha-anomers. This selectivity pattern parallels that of O-glycoside formation and eliminates the need to consider donor-acceptor hydrogen bonding in the formation of the O-glycosides.
Intermolecular asymmetric 1,3-dipolar cycloaddition of 2,2-dimethyl-3,4-dihydro-2H- pyrrole N-oxide and N-(benzylidene)methylamine N-oxide with optically active α, β-unsaturated esters 1,2,4 and 7-9 provided the corresponding diastereomers while chiral sugar lactones gave stereoselectively the cycloadducts 17a and 17b (in the case of dipolarophile 3) and 18 in (the case of the dipolarophile 6) with the acyclic nitrone B. The stereochemistry of the products has been established using high field nmr techniques. The regioselectivities of these reactions are inconsistent with FMO coefficients and are explained on the basis of charge distribution obtained through AM1 calculations. ...
Is donor-acceptor cialis side effects hydrogen bonding necessary for 4,6-O-benzylidene-directed beta-mannopyranosylation? We tested the use of a viral envelope protein gp64 transgenic mouse for the direct immunization of these membrane proteins displayed on BVs. The aim of this study has been to evaluate the reported preparedness and disposition by medical students in a Nigerian university toward the use of IT for medical education.. Long-term categorical auditory performance and speech intelligibility in Mandarin-speaking prelingually deaf children with early cochlear implantation in Taiwan. To explore the repeatability of lower-order and higher-order ocular aberrations measured in patients with keratoconus. Infectious complications following cialis sans ordonnance unrelated cord blood transplantation. The amphibian thyroid system is similar to that of mammals and other tetrapods. To describe the case of a person with schizophrenia and agenesis of the corpus cialis sans ordonnance livraison 48h ...
This project is supported by the Canadian Institutes of Health Research (award #111062), Alberta Innovates - Health Solutions, and by The Metabolomics Innovation Centre (TMIC), a nationally-funded research and core facility that supports a wide range of cutting-edge metabolomic studies. TMIC is funded by Genome Alberta, Genome British Columbia, and Genome Canada, a not-for-profit organization that is leading Canadas national genomics strategy with funding from the federal government. Maintenance, support, and commercial licensing is provided by OMx Personal Health Analytics, Inc. Designed by Educe Design & Innovation Inc. ...
Novel PKCs Do Not Act Upstream of p38 MAPK in Response to TNF. Having found that p38 MAPK and novel PKCs seemed to act independently in response to PMA, it was important to further explore this relationship in response to TNF. Initially, A549 cells were treated with bisindolylamide 1 or Go6976, and p38 MAPK phosphorylation was assessed. As with PMA, neither inhibitor had a significant effect on basal p38 MAPK phosphorylation. However, neither inhibitor had a significant effect on TNF-stimulated p38 MAPK phosphorylation (Fig. 7A), suggesting that, unlike with PMA, classic PKC is not upstream of p38 MAPK activation in response to TNF. To consolidate these data, the effect of rottlerin was determined. Although a small effect of rottlerin on TNF-stimulated p38 MAPK phosphorylation was observed (20%), this was not statistically significant (p , 0.1) (Fig. 7B). Thus, as with PMA, the TNF-stimulated activation of p38 MAPK is independent of novel PKCs, but unlike PMA, it is also independent of classic ...
Structure, properties, spectra, suppliers and links for: 7-[(2Z)-3-Chloro-2-buten-1-yl]-8-[(2E)-2-(2-hydroxybenzylidene)hydrazino]-3-methyl-3,7-dihydro-1.
Full text for this publication is not currently held within this repository. Alternative links are provided below where available. ...
Abstract. A single-step conversion of various N-vinyl and N-aryl amides to the corresponding pyridine and quinoline derivatives involves amide activation with trifluoromethanesulfonic anhydride in the presence of 2-chloropyridine followed by π-nucleophile addition to the activated intermediate and annulation. Compatibility of this chemistry with various functional groups is noteworthy.. ...
2-Benzylidene[3]ferrocenophane-1,3-diones were synthesized by condensation of substituted benzaldehydes and [3]ferrocenophane-1,3-dione with triethylamine as catalyst. Benzaldehydes bearing electron-accepting substituents gave bicyclic compounds as by-products; these were formed by extension of the three-membered bridged system to a seven-membered one. A correlation between ν(C=O) vibrations and σ+ constants of substituents was found. The UV and 1H-NMR spectra of the prepared compounds are commented.. ...
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4DTK: Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases.
0089]In those embodiments where the polyimine compound is defined by the formula II with n being equal to 2, the polyimine compounds may be referred to as heterocyclic bis-imine compounds. Specific examples of heterocyclic bis-imine compounds include N,N-bis(2-pyridylmethylidene)ethylenediamine, N-(2-pyridylmethylidene)-N-(benzylidene)ethylene diamine, N,N-bis(3-pyridylmethylidene)ethylene diamine, N-(3-pyridylmethylidene)-N-(benzylidene)ethylenediamine, N,N-bis(4-pyridylmethylidene)ethylenediamine, N-(4-pyridylmethylidene)-N-(benzylidene)ethylenediamine, N,N-bis(pyrazinylmethylidene)ethylenediamine, N,N-bis(2-pyrimidinylmethylidene)ethylenediamine, N,N-bis(3-pyridazinylmethylidene)ethylene diamine, N,N-bis(1-methyl-2-pyrrolylmethylidene)ethylene diamine, N,N-bis(1-methyl-2-imidazolylmethylidene)ethylenediamine, N,N-bis(1-methyl-3-pyrazolylmethylidene)ethylenediamine, N,N-bis(2-furylmethylidene)ethylene diamine, N,N-bis(3-furylmethylidene)ethylene diamine, ...
The invention provides a long acting curcumin derivative, preparation method and pharmaceutical use thereof, wherein said long acting curcumin derivative having the general structural formula disclosed herein, wherein R1 and R2 are hydrogen or methoxyl; R3 and R4 are each independently selected from C1-C50 alkyl. Compared with cuminoids, the inventive long acting curcumin derivative has a better release effect, a higher bioavailability and pharmaceutical activity, and thus can be useful for the treatment of diseases such as depression and cancer.
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2-(3-(5,6-Dichloro-1-ethyl-1,3-dihydro-3-(3-sulphonatobutyl)-2H-benzimidazol-2-ylidene)prop-1-enyl)-3-ethylbenzoxazolium 4-[[4-[2-(3-ethoxy-4-phenylmethoxy-phenyl)-1,3-thiazol-4-yl]phenyl]iminomethyl]-N,N-bis(3-methylsulfonyloxypropyl)aniline Eucalyptus maculata citriodora, ext., dehydrated Eicosane, 3-methyl- 1H-Indole, 3-(4,5-dihydro-3-(4-methoxyphenyl)-1-(2,4,6-trimethylphenyl)-1H-pyrazol-5-yl)-2-(4-methoxyphenyl)- Octadecanoic acid, reaction products with diethylenetriamine and triethylenetetramine, di-Et sulfate-quaternized benzo[1,3]dioxol-5-yl benzoate 5-chloro-9-thia-2,4,7-triazabicyclo[4.3.0]nona-2,4,7,10-tetraene Pyrrolo[4,3,2-de]quinoline-7,8-dione,1,3,4,5- tetrahydro-5-methyl- 4-(2-(2-((2-(2-(4-(Dihydroxyboryl)benzylidene)hydrazino)-1-methyl-2-oxoethyl)thio)propanoyl)carbohydrazonoyl)phenylboronic acid
1,3-Diethyl-5-(2-methoxybenzylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 3 was prepared by Knoevenagel condensation of 2-methoxybenzaldehyde 1 and N,N-diethylthiobarbituric acid 2 in ethanol using piperidine as a base [1,2].[...]
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The antioxidative properties of a novel curcumin analogue (2E,6E)-2,6-bis(3,5-dimethoxybenzylidene)cyclohexanone (MCH) were assessed by several in vitro models, including superoxide anion, hydroxyl radical and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging and PC12 cell protection from H2O2 damage. MCH displayed superior O2•− quenching abilities compared to curcumin and vitamin C. In vitro stability of MCH was also improved compared with curcumin. Exposure of PC12 cells to 150 µM H2O2 caused a decrease of antioxidant enzyme activities, glutathione (GSH) loss, an increase in malondialdehyde (MDA) level, and leakage of lactate dehydrogenase (LDH), cell apoptosis and reduction in cell viability. Pretreatment of the cells with MCH at 0.63-5.00 µM before H2O2 exposure significantly attenuated those changes in a dose-dependent manner. MCH enhanced cellular expression of transcription factor NF-E2-related factor 2 (Nrf2) at the transcriptional level. Moreover, MCH could mitigate intracellular
The reactions of amino- and formylimidazoles, and aminopyrimidinones are described. Conditions were found for the successful condensation of 5(4)-aminoimidazole-4(5)-carboxamide with a number of substituted benzaldehydes, to provide a series of novel 5(4)-N-benzylideneaminoimidazole-4(5)-carboxamides. Reaction of a subset of the benzylidene derivatives with sodium hydride furnished novel imidazo[1,5-a]quinazoline-3-carbox-amides in good yields, via an intramolecular cyclisation. Attempted mixed acid nitration of imidazo[1,5-a]quinazoline-3-carboxamide led only to amide hydrolysis to provide the carboxylic acid. High yielding conditions were sought for the synthesis of a formylimidazole by the selective partial reduction of commercially available 4,5-disubstituted imidazoles. Lithium triethoxy-aluminium hydride reduction of 1-benzyl-4,5-dicyanoimidazole gave a mixture of the isomeric monoaldehydes in a yield of 53%. Methyl 5(4)-formylimidazole-4(5)-carboxylate was formed by acidic hydrolysis of ...
TY - JOUR. T1 - Design and synthesis of highly constrained factor Xa inhibitors. T2 - Amidine-Substituted bis(benzoyl)-[1,3]-diazepan-2-ones and bis(benzylidene)-bis(gem-dimethyl)cycloketones. AU - Cui, Jian. AU - Crich, David. AU - Wink, Donald. AU - Lam, Matthew. AU - Rheingold, Arnold L.. AU - Case, David A.. AU - Fu, Wen Tao. AU - Zhou, Yasheen. AU - Rao, Mohan. AU - Olson, Arthur J.. AU - Johnson, Michael E.. PY - 2003/8/5. Y1 - 2003/8/5. N2 - Two conformationally constrained templates have been designed to provide selective inhibitors of the coagulation cascade serine protease, Factor Xa (FXa). The most active inhibitor, 2,7-bis[(Z)-p-amidinobenzylidene)]-3,3,6,6-tetramethylcycloheptanone, exhibits a Ki of 42 nM against FXa, with strong selectivity against thrombin (1000-fold), trypsin (300-fold) and plasmin (900-fold). With only two freely rotatable bonds, molecular modeling suggests that one amidine group is positioned into the S1 pocket, forming hydrogen bonds with the side chain of ...
149. Mugunthan G, Sriram D, Yogeeswari P, Ravindranathan Kartha KP. Synthetic analogues of mycobacterial arabinogalactan linkage-disaccharide part II: synthesis and preliminary screening of lipophilic O-alkyl glycosides. Carbohydr Res. 2011 346: 2401-5.. 148. Chitra, S., Paul, N., Muthusubramanian, S., Manisankar, P., Yogeeswari, P., Sriram, D. A facile synthesis of carbocycle-fused mono and bis-1,2,3-selenadiazoles and their antimicrobial and antimycobacterial studies. Eur J Med Chem. 2011, Nov;46(11):5465-72.. 147. Narang, R., Narasimhan, B., Sharma, S., Sriram, D., Yogeeswari, P., De Clercq, E., Pannecouque, C., Balzarini, J. Synthesis, antimycobacterial, antiviral, antimicrobial activities, and QSAR studies of nicotinic acid benzylidene hydrazide derivatives. Med. Chem. Res. 2011 In Press 146. Kantevari S, Yempala T, Surineni G, Sridhar B, Yogeeswari P, Sriram D. Synthesis and antitubercular evaluation of novel dibenzo[b,d]furan and 9-methyl-9H-carbazole derived ...
The coupling of o-bromobenzoic acid with terminal alkynes using 10% Pd/C-Et3N-CuI-PPh3 as a catalyst system leads to the synthesis of (Z)-3-alkylidenephthalides as the major product along with the traces of isocoumarin when the reaction was performed in 1,4-dioxane. The methodology afforded a range of compounds including (Z)-3-(4-(methylsulfonyl)benzylidene)isobenzofuran-1(3H)-one of potential pharmacological interest. (C) 2013 Elsevier Ltd. All rights reserved.. ...
Propiophenones of the formula I ##STR1## in which R1 is hydrogen or C1 -C4 -alkyl, --Si(CH3)3, allyl or benzyl, R2 is hydrogen, C1 -C8 -alkyl, C1 -C4 -alkyl which is substituted by C1 -C4 -alkoxy or --OH, --(CH2 --CH2 --O)n --R5 where n is 2 to 20 and R5 is H or C1 -C4 -alkyl, --Si(CH3)3, benzyl, C3 -C6 -alkenyl, C3 -C4 -alkynyl or 2-tetrahydrofuranyl, or R1 and R2 together are a C1 -C6 -alkylidene radical or a C2 -C6 -alkylidene radical which is substituted by hydroxyl, C1 -C4 -alkoxy or phenyl, a linear or branched C2 -C6 -alkanediyl radical, a benzylidene, cyclopentylidene or cyclohexylidene radical or a 2,2,2-trichloroethylidene, 2-furylmethylidene or dimethylsilylidene radical, R3 is phenyl which is unsubstituted or substituted by one or more --Cl, C1 -C4 -alkyl, C1 -C4 -alkoxy or C1 -C4 -alkylthio radicals, and is also benzoylphenyl, phenoxyphenol or phenylthiophenyl, R4 is C1 -C4 -alkyl, or phenyl which is unsubstituted or substituted by one or more --Cl, C1 -C4 -alkyl or C1 -C4 -alkoxy radicals,
Vijaya, S and Vasu, * and Gowda, Arjuna KV and Narasimhamurthy, T and Rathore, RS (2011) 4-(4-Chlorophenyl)-N-[(E)-4-(dimethylamino)benzylidene]-1,3-thiazol-2- amine. In: Acta Crystallographica Section E, 67 (Part 8). O2115-U1228. Vijaya, S (1998) The genetics of Mycobacterium tuberculosis. In: Journal of Genetics, 77 (2-3). pp. 123-128. Wolffe, Elizabeth J and Vijaya, S and Moss, Bernard (1995) A Myristylated Membrane Protein Encoded by the Vaccinia Virus L1R Open Reading Frame Is the Target of Potent Neutralizing Monoclonal Antibodies. In: Virology, 211 (1). pp. 53-63. Kalyani, P and Vijaya, S and Ramasarma, T (1992) Characterization of oxygen free radicals generated during vanadate-stimulated NADH oxidation. In: Molecular and Cellular Biochemistry, 111 (1-2). pp. 33-40. Ramasarma, T and Rasheed, BK and Vijaya, S and Puranam, RS and Shivaswamy, V and Gaikwad, AS and Kurup, CK (1992) Functions Of Cytochrome-C In Regulation Of Electron-Transfer And Protein Folding. In: Indian Journal of ...
The Notch1 receptor and signaling pathway is upregulated in HCC. The present study was conducted to evaluate the effect of mesenchymal stem cells (MSCs) and a ...
[Fe(L)2(H2O)2]-Y complex (where, L = ( Z)-2-((4-hydroxybenzylidene)-amino)benzoic acid) has been synthesized by Flexible Ligand (FL) method and characterized by chemical analysis (CHN, ICP-OES, TGA,...
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Studies fond of the synthesis of (Z)-5-benzylidene-4-arylpyrrol-2(5H)-ones from (Z)-3-aryl-3-haloenoic acids are described. Hz 2 13 NMR (CDCl3) 187.9 153.9 141 137.8 128.7 127.5 91.8 45 37 21.3 IR (neat) 1639 cm?1; HRMS (ES) m/z calcd for C12H16NO 190.1226 found 190.1168. This compound experienced NMR spectral properties which were consistent with those previously reported.11 4.1 3 (14b) This compound was prepared by the above procedure with the exception that 4-methoxyacetophenone was used in the reaction in which case a 98 % yield of a solid was obtained. This material exhibited the following physical properties: mp 59-63 °C; 1H NMR (CDCl3) 2.99 (broad s 6 3.82 (s 3 5.69 (d 12.6 Hz 1 6.89 (d 7.8 Hz 2 7.76 (d 12.6 Hz 1 and 7.89 (d 8.7 Hz 2 13 NMR (CDCl3) 187.4 161.9 153.8 133.2 129.4 113.3 91.7 55.3 45 37 IR (neat) 1664 cm?1; HRMS (ES) m/z calcd for C12H16NO2 206.1176 found 206.1189. This compound experienced NMR spectral properties which were consistent with those previously reported.11 4.1 1 ...
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Immunoprecipitation of N-SMase with antibody against Hsp60.(A) The active N-SMase fraction from Mono S was used for IP. The active fraction was mixed with the s
TY - JOUR. T1 - Interaction of benzylidene-anabaseine analogues with agonist and allosteric sites on muscle nicotinic acetylcholine receptors. AU - Arias, H. R.. AU - Xing, H.. AU - MacDougall, K.. AU - Blanton, M. P.. AU - Soti, F.. AU - Kern, W. R.. PY - 2009/5/1. Y1 - 2009/5/1. N2 - Background and purpose: Benzylidene-anabaseines (BAs) are partial agonists of the α7 nicotinic acetylcholine receptor (nAChR) but their mechanism(s) of action are unknown. Our study explores several possibilities, including direct interactions of BAs with the nAChR channel. Experimental approach: Functional and radioligand-binding assays were used to examine the interaction of two BA analogues, 3-(2,4-dimethoxybenzylidene)-anabaseine (DMXBA) and Its primary metabolite 3-(4-hydroxy-2-methoxybenzylidene)anabaseine (4OH-DMXBA) with both agonist and non-competitive antagonist (NCA)-bindlng sites on muscle-type nAChRs. Key results: Both BAs non-competitively inhibited ACh activation of human fetal muscle nAChRs and ...
The first objective of this thesis was to investigate effects of endocrine disruptors on the developing brain and gonads of bird embryos. The substances studied were the insecticide methoxychlor, and nine UV-filters (3-benzylidene camphor (3BC), 4 methyl benzylidene camphor (4MBC), benzophenone (BP) 1,2 and 3, 4 hydroxy benzophenone (4 HB), 4 dihydroxy benzophenone (4DHB), benzyl salicylate (BS), and ethyl-4-aminobenzoate Et-PABA)), commonly used in cosmetic products. Some of these substances have no estrogenic effect in vitro, but have been shown to be estrogenic in vivo. The PCB-mixture Clophen A50 is a well-known inducer of biotransformation enzymes and was co-administered with methoxychlor and the UV-filters 3BC and 4MBC.. Exposure to 3BC or 4MBC caused ovotestis formation and malformations of the Müllerian ducts in Japanese quail embryos. Co-exposure to one of these compounds and Clophen A50 enhanced the effects, indicating that Clophen A50 potentiates the effects of the UV-filters. ...
Trifluoromethanesulfonic Acid as Acylation Catalyst: Special Feature for C- and-or O-Acylation Reactions. . Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
Materials. Guanabenz was purchased from Research Biochemicals International (Natick, MA). Glucose 6-phosphate, glucose 6-phosphate dehydrogenase, NADP+, NG-nitro-l-arginine, l-arginine, d-arginine, dihydropteridine reductase from sheep liver, calmodulin, catalase, superoxide dismutase, and NADPH were purchased from Sigma Aldrich (St. Louis, MO). Male Wistar rats were purchased from Charles River Laboratories (Wilmington, MA). (6R)-5,6,7,8-Tetrahydro-l-biopterin (BH4) was purchased from Dr. Schirks Laboratory (Jona, Switzerland). The affinity-purified rabbit IgG against brain NOS used for immunoblotting nNOS was from BD Biosciences Transduction Laboratories (Lexington, KY). [Benzylidene carbon 14C]-labeled guanabenz (56 mCi/mmol) was custom-synthesized by Du Pont NEN (Boston, MA). l-[14C(U)]-Arginine (330.0 mCi/mmol) and 125I-labeled antibody against rabbit IgG were purchased from PerkinElmer Life and Analytical Sciences (Boston, MA).. Methods.In vitro inhibition assays. For studies on the ...
The synthesis of 4-[(E)-(-2,5- dimethoxybenzylidene)amino] benzoic acid Schiff base, SBDAB was carried out inorder to determine its inhibitory efficiency at higher temperature using weight loss and gasometric techniques. The results showed that the inhibition efficiency of the studied Schiff base increased with increase in temperature for the corrosion of mild steel which suggests chemisorption reaction mechanism. The negative free energy of adsorption obtained confirms a spontaneous adsorption of the Schiff base on the metal surface. The positive values of the heat of adsorption suggest an endothermic reaction. The positive values of the entropy of adsorption suggest a disordered system. The Langmuir adsorption Isotherm result showed a deviation from an ideal Langmuir adsorption isotherm equation, this is due to the interaction of the inhibitor molecules with one another. The inhibition efficiency of 35.20% and 35.31% was obtained for the weight loss and gasometric techniques respectively. The ...
Thioglycosides have proved to be useful, enzymatically stable analogs of glycosides for structural and mechanistic studies and their synthesis is considerably simplified through the use of thioglycoligases. As part of an investigation into the use of thioglycosides as potential pharmacological chaperones, and as components of glycoproteins and glycolipids, the syntheses of p-nitrophenyl 3-thio-β-D-galactopyranoside, phenyl 1,4-dithio-β-D-glucopyranoside, p-nitrophenyl 4-thio-β-D-mannopyranoside and p-nitrophenyl 2-acetamido-2-deoxy-4-thio-β-D-mannopyranoside are described.
Here we report a method for the preparation of anomerically pure β-S-glycopyranosides (1,2-trans-glycosides) from the corresponding peracetate donors. S-glycosylation was performed in CHCl3 at reflux in the presence of a catalytic amount of InBr3. Deacylation of the intermediate peracetates were achieved under Zemplén conditions. Five pyranose examples, monosaccharides D-glucose and D-galactose and disaccharides cellobiose, maltose, and lactose, were used as donors, and five thiols including an α/ω dithiol and Fmoc-L-cysteine were used as acceptors. Melting points, high res MS, [α]D and NMR data ((1)H and (13)C, including COSY, HSQC and HMBC) are reported for compounds not previously described ...
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Wear a self-contained breathing apparatus in pressure-demand, MSHA/NIOSH (approved or equivalent), and full protective gear. During a fire, irritating and highly toxic gases may be generated by thermal decomposition or combustion. Extinguishing media: Use agent most appropriate to extinguish fire. In case of fire use water spray, dry chemical, carbon dioxide, or appropriate foam ...
HMN-214 inhibits polo-like and cyclin-dependent kinase activity, has potent antimicrotubular effects and results in profound apoptosis and antitumor activity in a broad spectrum of human xenografts.
Sphingomyelin (d18:1/18:0) or SM(d18:1/18:0) is a type of sphingolipid found in animal cell membranes, especially in the membranous myelin sheath which surrounds some nerve cell axons. It usually consists of phosphorylcholine and ceramide. SM(d18:1/18:0) consists of a sphingosine backbone and a stearic acid chain. In humans, sphingomyelin is the only membrane phospholipid not derived from glycerol. Like all sphingolipids, SM has a ceramide core (sphingosine bonded to a fatty acid via an amide linkage). In addition, it contains one polar head group, which is either phosphocholine or phosphoethanolamine. The plasma membrane of cells is highly enriched in sphingomyelin and is considered largely to be found in the exoplasmic leaflet of the cell membrane. However, there is some evidence that there may also be a sphingomyelin pool in the inner leaflet of the membrane. Moreover, neutral sphingomyelinase-2, an enzyme that breaks down sphingomyelin into ceramide, has been found to localize exclusively to ...
Purpose : Presynaptic modulation of γ-aminobutyric acid (GABA) release by an alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist promotes retinal ganglion cell (RGC) survival and function, as suggested by a previous study on a chronic glaucomatous model from our laboratory. However, the role of excitatory and inhibitory amino acid receptors and their interaction with α7-nAChR in physiological and glaucomatous events remains unknown. Methods : Using patch clamp techniques, the GABA-elicited membrane current and miniature excitatory postsynaptic currents (mEPSCS) of RGCs and the NMDA-gated current (INMDA) were detected in rat retinal slices. The expression of the GABAA receptor and NMDA receptors (NMDAR) subunit NR1, NR2A and NR2B in retinas were detected using western blotting and immunostaining. Results : Whole-cell patch-clamp recordings from RGCs revealed profound changes in the GABAA receptor and NMDAR properties under glaucoma conditions. The α7-nAChR specific agonist PNU-282987 ...
It has been previously acknowledged that perchlorate salts may be beneficial for the formation of 1,2-cis glycosides. Here, we demonstrate the effectiveness of silver (I) perchlorate as a powerful promoter of glycosyl thioimidate activation. Improved 1,2-cis selectivity was obtained, compared against that obtained with other silver (I) salts, including commonly-used trilate. The use of a combination of silver (I) perchlorate and methyl sulfenyl bromide to activate thioglycosides was also investigated. The cooperative use of these activation protocols was applied to a one-pot, two-step sequential activation, using thioimidate and thioglycoside building blocks ...
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Les Laboratoires Servier (Servier) in France is developing conformationally restricted acetylcholine analogues as potential agents for the treatment of
This influence on cortical function has been exemplified by the work of Jason Tregellas and colleagues. These researchers examined the effects of DMXB-A, a novel alpha-7 partial agonist, on the brains default network in people with schizophrenia. Function of the default network, which is likely a major contributor to the intrinsic neuronal activity that accounts for 60-80% of the brains energy use, is different in people with schizophrenia ...
Bardag-Gorce, F., Yuan, Q.X., Li, J., French, B.A., Fang, C., Ingelman-Sundberg, M., French, S.W., 2000. The effect of ethanol-induced cytochrome p4502E1 on the inhibition of proteasome activity by alcohol. Biochem. Biophys. Res. Commun. 279, 23-29.. Bondoc, F.Y., Bao, Z., Hu, W.Y., Gonzalez, F.J., Wang, Y., Yang, C.S., Hong, J.Y., 1999. Acetone catabolism by cytochrome P450 2E1: studies with CYP2E1-null mice. Biochem. Pharmacol. 58, 461-463.. Cederbaum, A.I., 2014. Methodology to assay CYP2E1 mixed function oxidase catalytic activity and its induction. Redox Biol. 2C, 1048-1054.. Cheng, J., Chen, C., Kristopher, K.W., Manna, S.K., Scerba, M., Friedman, F.K., Luecke, H., Idle, J.R., Gonzalez, F.J., 2013. Identification of 2-piperidone as a biomarker of CYP2E1 activity through metabolomic phenotyping. Toxicol. Sci. 135, 37-47.. Cheung, C., Gonzalez, F.J., 2008. Humanized mouse lines and their application for prediction of human drug metabolism and toxicological risk assessment. J. Pharmacol. Exp. ...
Significant pharmaceutical innovations and progresses have occurred in oncology treatments and patients management. Recent signal transduction inhibitor agents having a strong anti-tumour specificity are able to disrupt signal pathways mediating cancer cell proliferation and efficiently prevent tumour growth. Signal transduction inhibitors include imatinib, sunitinib, nilotinib, dasatinib, sorafenib and other tyrosine kinase blockers currently under investigation. But other chemotherapeutic drugs such as antimetabolites (methotrexate, 5-Fluorouracil), mitotic spindle inhibitors (vincristine, vinorelbine), antibiotic inhibitors of topoisomerases (etoposide, topotecan) etc. are also increasingly used in oncology. As a consequence, cancer patients are living longer, and the amount of consumption of these classes of drugs has grown accordingly. In parallel, the amount of anticancer drug residues released into the environment has increased. Indeed, most anticancer drugs are eliminated by urines or ...
TY - JOUR. T1 - Aryl-Aryl Coupling of Salicylic Aldehydes through Oxidative CH-activation in Nickel Salen Derivatives. AU - Yankin, Andrei N.. AU - Lukyanov, Daniil A.. AU - Beletskii, Evgenii V.. AU - Bakulina, Olga Yu. AU - Vlasov, Petr S.. AU - Levin, Oleg V.. PY - 2019/8/12. Y1 - 2019/8/12. N2 - The preparative electrosynthetic procedure for gram-scale preparation of symmetric 4,4′-dihydroxy-3,3′-diformylbiphenyls from salicylic aldehydes via the intermediate formation of ethylene-bridged bis((2-hydroxybenzylidene)imino)nickel (II) complexes is reported for the first time. This procedure represents a practical route to the variety of rare bisphenol derivatives. The electrochemical aryl-aryl coupling via an oxidative CH - activation in NiSalens is exploited for facile and selective C−C bond formation.. AB - The preparative electrosynthetic procedure for gram-scale preparation of symmetric 4,4′-dihydroxy-3,3′-diformylbiphenyls from salicylic aldehydes via the intermediate formation ...
Enzymes are immobilized by dissolving in water a photo-crosslinking resin containing stilbazolium groups, vinyl alcohol units and vinyl acetate units, adding an enzyme to the resultant aqueous solution and exposing the enzyme-containing resin solution to light to induce a crosslinking reaction of the photo-crosslinking resin and produce a polymer containing the enzyme entrapped therein.
[VO(sal-L-tryp)(H2O)] (1, sal-L-tryp = N-salicylidene-L-tryptophanate) was used as a precursor to produce the new complexes [VO(sal-L-tryp)(MeATSC)].1.5C(2)H(5)OH [2, MeATSC = 9-Anthraldehyde-N(4)-methylthiosemicarbazone], [VO(sal-L-tryp)(N-ethhymethohcarbthio)]center dot H2O [3, N-ethhymethohcarbthio = (E)-N-ethyl-2-(4-hydroxy-3-methoxybenzylidene)-hydrazinecarbothioamide] and [VO(sal-L-tryp)(acetylethTSC)]center dot C2H5OH {4, acetylethTSC = (E)-N-ethyl-2-[1-(thiazol-2-yl) ethylidene]hydrazinecarbothioamide} by reaction with the respective thiosemicarbazone. The chemical and structural properties of these ligands and complexes were characterised by elemental analysis, ESI-MS, FTIR, UV/Vis, ESR and H-1 and C-13 NMR spectroscopy and X-ray crystallography. Dimethyl sulfoxide (DMSO) and [D-6]DMSO solutions of 1-4 were oxidised in air to produce vanadium(V) species, which were verified by ESI-MS and V-51 NMR spectroscopy. The anticancer properties of 2-4 were examined with three colon cancer cell lines,
BioAssay record AID 147531 submitted by ChEMBL: Inhibitory activity against schyphostatin of neutral sphingomyelinase (N-SMase) from bovine brain microsome.
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1-(4-Fluoro-phenyl)-piperidin-4-one/ACM116247984 can be provided in Alfa Chemistry. We are dedicated to provide our customers the best products and services.
TY - JOUR. T1 - A synthetic curcuminoid derivative inhibits nitric oxide and proinflammatory cytokine synthesis. AU - Tham, Chau Ling. AU - Liew, Choi Yi. AU - Lam, Kok Wai. AU - Mohamad, Azam Shah. AU - Kim, Min Kyu. AU - Cheah, Yoke Kqueen. AU - Zakaria, Zainul Amirudin. AU - Sulaiman, Mohd Roslan. AU - Lajis, Nordin H.. AU - Israf, Daud A.. PY - 2010/2/25. Y1 - 2010/2/25. N2 - Curcumin is a highly pleiotropic molecule with significant regulatory effects upon inflammation and inflammatory related diseases. However curcumin has one major important limitation in which it has poor bioavailability. Design of synthetic structural derivatives of curcumin is but one approach that has been used to overcome its poor bioavailability while retaining, or further enhancing, its drug-like effects. We have synthesized a series of curcumin analogues and describe the effects of 2,6-bis-4-(hydroxyl-3-methoxy-benzylidine)-cyclohexanone or BHMC upon nitric oxide and cytokine synthesis in cellular models of ...
Hendrickson, L. M., Zhao-Shea, R., & Tapper, A. R. (2009). Modulation of Ethanol Drinking-in-the-Dark by Mecamylamine and Nicotinic Acetylcholine Receptor Agonists in C57BL/6J Mice. Psychopharmacology, 204, 563-572.
Schneider, JS (2003). „The Subtype-Selective Nicotinic Acetylcholine Receptor Agonist SIB-1553A Improves Both Attention and Memory Components of a Spatial Working Memory Task in Chronic Low Dose 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine-Treated Monkeys". Journal of Pharmacology and Experimental Therapeutics. 306 (1): 401-6. PMID 12721323. doi:10.1124/jpet.103.051912 ...
Yadav VR, Vilekar P, Awasthi S, Awasthi V. Hemorrhage-induced interleukin-1 receptor pathway in lung is suppressed by 3,5-bis(2-fluorobenzylidene)-4-piperidone in a rat model of hypovolemic shock. Artif Organs. 2014 Aug;38(8):675-83. doi: 10.1111/aor.12305. Epub 2014 Apr 22. PubMed PMID: 24749913; PubMed Central PMCID: PMC4146623.. Awasthi S. Toll-like receptor-4 modulation for cancer immunotherapy. Front Immunol. 2014 Jul 25;5:328. doi: 10.3389/fimmu.2014.00328. eCollection 2014. Review. PubMed PMID: 25120541; PubMed Central PMCID: PMC4110442. Awasthi S, Anbanandam A, Rodgers KK. Structure of a TLR4-interacting SPA4 peptide. RSC Adv. 2015;5(35):27431-27438. PubMed PMID: 25870755; PubMed Central PMCID: PMC4392768. Narasaraju T, Shukla D, More S, Huang C, Zhang L, Xiao X, Liu L. Role of microRNA-150 and glycoprotein nonmetastatic melanoma protein B in angiogenesis during hyperoxia-induced neonatal lung injury. Am J Respir Cell Mol Biol. 2015 Feb;52(2):253-61. doi: 10.1165/rcmb.2013-0021OC. PubMed ...
Application of an electric field to liquid crystalline film forming imines with negative dielectric anisotropy, such as N-(4-methoxybenzylidene)-4-butylaniline (MBBA, 1), results in the expulsion of compounds that do not participate in the formation of the liquid crystalline phase. Furthermore, amines and aromatic aldehydes undergo component exchange with the imine by generating constitutional dynamic libraries. The strength of the electric field and the duration of its application to the liquid crystalline film influence the release rate of the expelled compounds and, at the same time, modulate the equilibration of the dynamic libraries. The controlled release of volatile organic molecules with different chemical functionalities from the film was quantified by dynamic headspace analysis. In all cases, higher headspace concentrations were detected in the presence of an electric field. These results point to the possibility of using imine-based liquid crystalline films to build devices for the ...
United States Patent 3,480,635 N-PIPERIDYL SUBSTITUTED PHENYLENEDIAMINES Elmar R. Altwicker, Somerville, N.J., assignor to Universal Oil Products Company, Des Plaines, 111., a cor poration of Delaware No Drawing. Filed Sept. 28, 1966, Ser. No. 582,547 Int. Cl. C07d 29/10, 29/28 US. Cl. 260293 7 Claims ABSTRACT OF THE DISCLOSURE Novel N-piperidyl substituted phenylenediamines can be prepared by reductively alkylating a nitro or aminosubstituted phenylamine with a piperidone. These compounds are useful as antiozonants and antioxidants. This invention relates to a new class of compounds, to the preparational process therefor, and to compositions containing such compounds which are stabilized against deterioration caused by the action of ozone or oxygen. More particularly, this invention relates to N- piperidyl substituted phenylenediamines, The novel compounds of this invention may be represented by the following general formula: H -N-R, Rr-N where R, is a piperidyl radical of the formula: R, R ...
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Cuomo, J., Appendino, G., Dern, A., Schneider, E., McKinnon, T., Brown, M., Togni, S. and Dixon, B. (2011). Comparative Absorption of a Standardized Curcuminoid Mixture and Its Lecithin Formulation. J. Nat. Prod., 74(4), pp.664-669 ...
Learn more about dimethyl-4-2-piperidin-4-yl-ethyl-pyridin-2-yl-amine-dihydrochloride. We enable science by offering product choice, services, process excellence and our people make it happen.
Expression of PPP1R8 (ard-1, ARD1, NIPP-1, NIPP1, PRO2047) in vagina tissue. Antibody staining with HPA027406, HPA027417 and HPA027452 in immunohistochemistry.
Recently, several universities including the University of Saskatchewan initiated drug design and discovery programs to meet the shift in emphasis to translational research by the major funding organizations. The nascent Drug Design and Discovery Research Group at the University of Saskatchewan initiated an anticancer drug discovery program where one of the active projects focused on the development of curcumin analogues containing the 1,5-diaryl-3-oxo-1,4-pentadienyl group as anticancer agents. This became my Ph. D. dissertation research. My current work identifies the inadequacy in the current drug design and discovery model and provides initial direction for the future design of the curcumin analogues with better pharmacokinetic and pharmacodynamic properties. A battery of pharmacokinetic tests on NC 2083, a curcumin analogue that exhibits high in vitro efficacy but does not show any effect in vivo, suggested low permeability, high plasma protein binding and rapid partitioning into RBC as the ...
This suggestion is experimental, high-risk, and certainly not for everyone. If youre nursing or pregnant, or your brain is still developing, I would avoid nicotine like the plague.. But nicotine is one of the most robust nootropics. It also stacks remarkably well with modafinil. Thats why both drugs are at the top of my list of the best nootropics (http://www.brainprotips.com/best-nootropics-2016).. Heres what one researcher has to say about nicotine:. "To my knowledge, nicotine is the most reliable cognitive enhancer that we currently have, bizarrely," said Jennifer Rusted, professor of experimental psychology at Sussex University in Britain when we spoke. "The cognitive-enhancing effects of nicotine in a normal population are more robust than you get with any other agent. With Provigil, for instance, the evidence for cognitive benefits is nowhere near as strong as it is for nicotine.". Why does nicotine work so well? Its a potent nicotinic acetylcholine receptor agonist. Nicotinic ...
Schneider, JS (July 2003). "The Subtype-Selective Nicotinic Acetylcholine Receptor Agonist SIB-1553A Improves Both Attention and Memory Components of a Spatial Working Memory Task in Chronic Low Dose 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine-Treated Monkeys". Journal of Pharmacology and Experimental Therapeutics 306 (1): 401-6. PMID 12721323. doi:10.1124/jpet.103.051912. Cite uses deprecated parameter ...
As far as the synergy, I would think that most would be already taking the CoQ-10, resveratrol, B-vitamins and green tea.. Curcumin-soy formulation may boost absorption 60-fold: Indena study - Nutra USA, 4/6/11 - Curcumin has been a sort of forbidden fruit for biomedical research, since its poor oral bioavailability has substantially hampered clinical development, despite the very promising indications of the preclinical research ... The volunteers received five (low-dose - 209 mg total curcuminoids) or nine (high-dose - 376 mg total curcuminoids) hard-shell capsules of either the soybean-based phospholipid-curcumin formulation (Meriva) or five capsules of a non-formulated curcuminoid mixture containing 1799 mg of curcuminoids ... Total curcuminoid absorption was about 29-fold higher for Meriva than for its corresponding unformulated curcuminoid mixture, but only phase-2 metabolites could be detected, and plasma concentrations were still significantly lower than those required for the ...
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2BYR: Structures of Aplysia Achbp Complexes with Nicotinic Agonists and Antagonists Reveal Distinctive Binding Interfaces and Conformations.
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Nicotine is a potent parasympathomimetic alkaloid found in the nightshade family of plants (Solanaceae) and a stimulant drug. It is a nicotinic acetylcholine receptor agonist. It is made in the roots and accumulates in the leaves of the plants. It constitutes approximately 0.6-3.0% of the dry weight of tobacco[1] and is present in the range of 2-7 µg/kg of various edible plants.[2] It functions as an antiherbivore chemical; consequently, nicotine was widely used as an insecticide in the past[3][4] ...
Twenty-three monoketone derivatives of curcumin were synthesized to investigate the synergy with fluconazole against fluconazole-resistant Candida spp. The minimal inhibitory concentration (MIC80) and the fractional inhibitory concentration index (FICI) of the antifungal synergist fluconazole were measured a
Title:Design and Synthesis of Curcumin-Like Diarylpentanoid Analogues as Potential Anticancer Agents. VOLUME: 11 ISSUE: 3. Author(s):Elahe Qudjani, Maryam Iman, Asghar Davood, Mahdi F. Ramandi and Abbas Shafiee. Affiliation:Department of Medicinal Chemistry, Faculty of Pharmacy, Pharmaceutical Sciences Branch, Islamic Azad University, Tehran, Iran, Tehran, 19419, Iran.. Keywords:Cancer, curcumin, docking, MTT, 4-piperidone, synthesis.. Abstract:Background: Curcumin is a polyphenolic natural compound with multiple targets that used for the prophylaxis and treatment of some type of cancers like cervical and pancreatic cancers. Some recent patent for curcumin for cancer has also been reviewed. Objective: In this study, ten new curcumin derivatives were designed and synthesized and their cytostatic activity evaluated against the Hela and Panc cell lines that some of them showed more activity than curcumin. Method: In the present study, a series of mono-carbonyl derivatives of curcumin were designed ...
Cisplatin is an anti-cancer drug effective against several cancers which can produce the serious side-effect of hearing loss. Curcumin, a natural plant compound, can increase the activity of cisplatin against cancer and counteract cisplatins effect against hearing. Because curcumin exhibits poor bioavailability, there is considerable interest in developing synthetic curcumin analogs (curcuminoids) that are more soluble and which retain anti-cancer activity and otoprotective function. This study investigated whether two curcuminoids, EF-24 and CLEFMA, increase the cytotoxic and ototoxic effects of cisplatin against the lung cancer cell line, A549, and the colorectal cancer cell line, Caco2. Cytotoxicity was measured by using the colorimetric 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Ototoxicity was quantified by measuring hearing thresholds acquired by the auditory evoked potential technique in a zebrafish (Danio rerio) model. The results of this study indicate that a
Analogs of 3-Benzylideneanabaseine. Syntheses of DMXBA and two O-demethylated analogs (Fig. 1A) were described by Kem et al. (2004). The dihydrochloride salts were dissolved in the appropriate physiological saline, and stock solutions were aliquoted and frozen. Because DMXBA is light-sensitive, the compounds were not exposed to strong light.. Isolation ofXenopus laevisOocytes.X. laevis frogs were kept in tanks of dechlorinated tap water on a 10-h light/14-h dark cycle at 19°C and fed a diet of AquaMax 500 grower (Purina Mills, St. Louis, MO) three times per week. Frogs were anesthetized by immersion in ice-cold 0.12% 3-aminobenzoic acid ethyl ester for 20 min. After removal through a small incision in the frogs abdomen, ovarian lobes were placed in modified Barths solution (MBS) containing 88 mM NaCl, 1 mM KCl, 2.4 mM NaHCO3, 10 mM HEPES, 0.82 mM MgSO4, 0.33 mM Ca(NO3)2, and 0.91 mM CaCl2, pH 7.5.. Ovarian lobes were manually dissected into clumps of four to ten oocytes and were then ...
This 202 word essay is about Smoking, Tobacco, Nicotinic agonists, Habits, Summer, Cigarette, Nicotine, Tar, Cannabis smoking, Health effects of tobacco. Read the full essay now!
Nectar and pollen foragers treated with 0.21 or 2.16 ng of the nAChR agonist imidacloprid showed a significant decrease in their SR 1 h after treatment. They extended their proboscises only for higher concentration sucrose solutions as compared with control bees. Analyses of two measures of SR yielded the same results. Treated bees had elevated SRT and lower total PER bee-1 (lower gustatory response scores) compared with controls. In addition, there were dose-dependent differences in the effects of imidacloprid on nectar and pollen foragers. These foragers were defined by what they were collecting immediately before testing. Both doses of imidacloprid significantly reduced SR in nectar foragers. Pollen foragers only reduced their SR in response to the higher dose. We also provide the first detailed results showing that imidacloprid metabolites can affect honey bee recruitment dances. Imidacloprid has a metabolic half-life of 4-5 h (Suchail et al., 2004a). When tested 24 h after imidacloprid ...
Myocardial ischemia/reperfusion (I/R) induces inflammatory response that may lead to remote vascular injury. Vagal nerve elicits the cholinergic anti-inflammatory pathway by activating α7 nicotinic ac
Levamisole was originally used as an anthelmintic to treat worm infestations in both humans and animals. Levamisole works as a nicotinic acetylcholine receptor agonist that causes continued stimulation of the parasitic worm muscles, leading to
Osteoarthritis is the most frequent joint disease worldwide. Patients with osteoarthritis mostly use non-steroidal anti-inflammatory drugs (NSAIDs) such as diclofenac sodium for reducing pain. Diclofenac sodium frequently disturbs the liver function. Curcuminoid has an anti-inflammatory activity and some references state that curcuminoid protects the liver function. The purpose of this study was to compare the effects of curcuminoid from Curcuma domestica Val. rhizome extract and diclofenac sodium on the liver function of patients with osteoarthritis. A total of 80 patients with knee osteoarthritis were enrolled. Subjects were divided randomly into two groups; a group received 30 mg of curcuminoid from C. domestica Val. 3 times daily (curcuminoid group) and the other received 25 mg of diclofenac sodium 3 times daily (diclofenac group). Assessment of results includes serum levels of aspartate aminotransferase (AST) and alanine aminotransferase (ALT) performed before and after 4 weeks of ...
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In a method of developing muscle mass in a mammal, nicotine or nicotine acetylcholine receptor agonist (nAChR) is administered in combination with exercise to stimulate, recruit and mobilize muscle cells to a specific muscle mass.
TY - JOUR. T1 - Protic acid catalyzed stereoselective glycosylation using glycosyl fluorides. AU - Jona, Hideki. AU - Mandai, Hiroki. AU - Chavasiri, Warinthorn. AU - Takeuchi, Kazuya. AU - Mukaiyama, Teruaki. PY - 2002/3/14. Y1 - 2002/3/14. N2 - A catalytic and stereoselective glycosylation of various glycosyl acceptors, such as methyl glycosides, thioglycosides, or a disarmed glycosyl fluoride, with benzyl-protected armed glycosyl fluoride was successfully carried out by using various protic acids in the presence of MS 5A. In the cases when trifluoromethanesulfonic acid (TfOH) or perchloric acid (HClO4) was used in diethyl ether (Et2O), α-glycosides were obtained as major products, while β-stereoselectivity was observed when tetrakis(pentafluorophenyl)boric acid [HB(C6F5)4] was used in a mixed solvent of trifluoromethylbenzene (BTF)-pivalonitrile (tBuCN) = 5:1. Stereoselectivity of this glycosylation was controlled by the properties of counter anions of the catalyst as well as by those of ...
Five cases of severe neutropenia (neutrophil counts < 0.5 per 109 cells/L) associated with exposure to cocaine and levamisole, an antihelimithic agent no longer available in Canada, were identified in Alberta in 2008. Alberta and British Columbia (BC) public health officials issued an advisory and urged health care professionals to report cases to public health. This paper presents the findings of the public health investigations. Cases were identified prospectively through reporting by clinicians and a retrospective review of laboratory and medical examiners data from January 1, 2006 to March 31, 2009. Cases were categorized as confirmed, probable or suspect. Only the confirmed and probable cases are included in this paper. We compare cases of severe neutropenia associated with tainted cocaine (NATC) identified in Alberta and BC between January 1, 2008 to March 31, 2009. Of the 42 NATC cases: 23(55%) were from Alberta; 19(45%) were from British Columbia; 57% of these cases reported crack cocaine use
Nicotine. Nicotine is a potent parasympathomimetic alkaloid found in the nightshade family of plants. It acts as a nicotinic acetylcholine receptor agonist. It is made in the roots and accumulates in the leaves of the plants. It constitutes approximately 0.6-3.0% of the dry weight of tobacco and is present in the range of 2-7 µg/kg of various edible plants. It functions as an antiherbivore chemical; therefore, nicotine was widely used as an insecticide in the past and nicotine analogs such as imidacloprid are currently widely used. In smaller doses, the substance acts as a stimulant in mammals, while high amounts can be fatal. This stimulant effect is likely a major contributing factor to the dependence-forming properties of tobacco smoking. According to the American Heart Association, nicotine addiction has historically been one of the hardest addictions to break, while the pharmacological and behavioral characteristics that determine tobacco addiction are similar to those determining ...
I read recently an article claiming that people could become dependent upon heroin from their first exposure to the drug. While it is entirely credible that someone may discover that they like the drug upon first using it and then continue to use it in a pattern that eventually leads to dependence, it is entirely…
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... are alkene derivatives of benzene. They are primarily divided into two groups: Styrenes (one benzene) ... Dibenzylideneacetone Aurone Benzylidene Compounds at the US National Library of Medicine Medical Subject Headings (MeSH). ... 6-O-benzylidene-glucopyranose is a glucose molecule whose 4- and 6-OH groups are protected by being bound to a benzylic carbon ... Stilbenes (two benzenes) Benzylidene is also used to describe a type of protecting group in synthetic organic chemistry of the ...
... benzylidene compounds MeSH D02.455.426.559.389.150.700 --- stilbenes MeSH D02.455.426.559.389.150.700.050 --- 4-acetamido-4'- ... trialkyltin compounds MeSH D02.691.850.900.910 --- triethyltin compounds MeSH D02.691.850.900.950 --- trimethyltin compounds ... mustard compounds MeSH D02.455.526.728.468 --- mustard gas MeSH D02.455.526.728.650 --- nitrogen mustard compounds MeSH D02.455 ... bephenium compounds MeSH D02.092.877.096.333 --- bretylium compounds MeSH D02.092.877.096.333.150 --- bretylium tosylate MeSH ...
... β-unsaturated carbonyl compound with an imine in the presence of a nucleophile. The reaction product is an allylic amine. The ... 4-chloro-benzylidene)-benzenesulfonamide with methyl vinyl ketone (MVK) in cyclopentyl methyl ether and toluene at -15°C. In ... with the aid of bifunctional chiral BINOL and phosphinyl BINOL compounds, for example in the reaction of n-( ...
It is a benzylidene camphor derivative, many of which are known for their excellent photostability. Although there are a few ... Ecamsule (USAN, trade name Mexoryl SX, INCI terephthalylidene dicamphor sulfonic acid) is an organic compound which is added to ... Benzylidene camphor and dibenzoylmethane derivatives". Int J Cosmet Sci. 10 (2): 53-62. doi:10.1111/j.1467-2494.1988.tb00002.x ...
... is a heterocyclic chemical compound which is a type of flavonoid. There are two isomers of the molecule, with (E)- and ( ... The molecule contains a benzofuran element associated with a benzylidene linked in position 2. In aurone, a chalcone-like group ... aurone glucoside and other aromatic compounds of Gomphrena agrestis with biological activity" (PDF). Zeitschrift für ...
... (C6H5CHO) is an organic compound consisting of a benzene ring with a formyl substituent. It is the simplest ... With diols, including many sugars, benzaldehyde condenses to form benzylidene acetals. Uses[edit]. Benzaldehyde is commonly ... In industrial settings, benzaldehyde is used chiefly as a precursor to other organic compounds, ranging from pharmaceuticals to ... Beltran-Garcia, Miguel J.; Estarron-Espinosa, Mirna; Ogura, Tetsuya (1997). "Volatile Compounds Secreted by the Oyster Mushroom ...
Electron-rich aromatic compounds, such as phenols, anilines, and various aromatic heterocycles, can be brominated using NBS. ... Binkley, R. W.; Goewey, G. S.; Johnston, J. (1984). "Regioselective ring opening of selected benzylidene acetals. A ... Side reactions include the formation of α-bromoketones and dibromo compounds. These can be minimized by the use of freshly ... Collective Volume, 6, p. 190 Stotter, P. L.; Hill, K. A. (1973). "α-Halocarbonyl compounds. II. Position-specific preparation ...
A mechanistic study by Plenio and coworkers in 2012 suggested that the Zhan compounds, like other Hoveyda-type catalysts, ... As with other Grubbs-type catalysts with modified chelating benzylidenes, after one catalytic turnover, the chelate is no ... "Origins of Initiation Rate Differences in Ruthenium Olefin Metathesis Catalysts Containing Chelating Benzylidenes". J. Am. Chem ... developed a model that could rationalize initiation rates of ruthenium olefin metathesis catalysts with chelated benzylidenes, ...
... the compounds are chiral. Sulfinamides are amides of sulfinic acid (RS(O)OH). Tert-Butanesulfinamide, p-toluenesulfinamide, and ... BENZYLIDENE)-p-TOLUENESULFINAMIDE". Organic Syntheses. 77: 50. CS1 maint: Multiple names: authors list (link) ; Collective ...
... , an organic compound belonging to the esters, lactones, alcohols and butenolides classes, is a yellow crystalline ... Ewan achieved the synthesis of this side-product and characterized it as the 5-benzylidene-4-hydroxy-3-phenylfuran-2(5H)-one. ... Yet vulpinic acid - as well as many of its derivatives - is a cytotoxic compound. Since pulvinones exhibit a lower cytotoxicity ... The aspulvinone terminology also incorporates a letter, indicating the order of chromatographic elution of these compounds ( ...
In H. sapiens, ODCase has been inhibited by halide compounds derived from UMP (e.g., 5-FUMP, 5-BrUMP, 5-IUMP, and 6-IUMP.) In ... 6-dihydroxipyridine-4-carboxylic acid and 3-benzylidene-2,6-dioxo-1,2,3,6-tetrahydropyridine-4-carboxylic acid. Union enthalpy ...
... (also known as alane or alumane) is an inorganic compound with the formula AlH3. It is a colourless ... doi:10.1016/S0040-4039(00)76929-2. Takano, S.; Akiyama, M.; Sato, S.; Ogasawara, K. (1983). "A Facile Cleavage of Benzylidene ... M.; Osipov, O. R. (1968). "Physicochemical Properties and Structure of Complex Compounds of Aluminium Hydride". Russian ... As a Hydrogen Storage Compound". doi:10.2172/899889. Aluminium Hydride on EnvironmentalChemistry.com Chemical Database Hydrogen ...
The material also include inexpensive commercially available compounds. The elastomer molecules were tweaked, making the bonds ... This process has been demonstrated with dicyclopentadiene (DCPD) and Grubbs' catalyst (benzylidene-bis(tricyclohexylphosphine) ...
These building blocks have been employed in the asymmetric synthesis of numerous biologically active compounds. The first N- ... Benzylidene-p-toluenesulfinamide. Regeneration of the Sulfinimine Precursor". Journal of Organic Chemistry. 60: 7037. doi: ... "Asymmetric Synthesis of β-Amino Carbonyl Compounds with N-Sulfinyl β-Amino Weinreb Amides". Journal of Organic Chemistry. 70: ...
Treatment of these compounds with TBAF invokes a ring-expansion that provides the corresponding benzazepines. One variation of ... 10.1016/j.tet.2008.12.059 Unprecedented regio and stereocontrol in Povarov reaction of benzylidene-(3-nitrophenyl)amine Paul J ... The imine in this organic reaction is a condensation reaction product from an aniline type compound and a benzaldehyde type ... a dirhodium catalyst effects diazo decomposition from silyl enol ether diazo compound to yield a donor/acceptor cyclopropene. ...
Suitable tripodal compounds, such as trimesic acid and nitrilotriacetic acid, can be converted directly to trisoxazolines. The ... Improving the Enantioselectivity in the Asymmetric Michael Addition of Indole to Benzylidene Malonate". The Journal of Organic ... homochiral ligands with C3 rotational symmetry and the modular approach typically being used to give asymmetric compounds (C1 ...
Some compounds are known to destroy melanocytes; this mechanism of action is often used to remove the remaining pigmentation in ... 2009). "Synthesis and evaluation of 5-benzylidene(thio)barbiturate-β-D-glycosides as mushroom tyrosinase inhibitors" (PDF). ... The relative activity (RA) of a compound under investigation is its activity divided by the activity of the positive control; ... In contrast, a study that examined the effect of glutathione and related compounds in-vitro found that glutathione monoethyl ...
... benzylidene sorbitol compounds; talc, polyvinyl Cyclohexane; and organic dicarboxylic acids such as oxalic acid, 1,2- ... PROCEDURE FOR COMPOUNDING POLYPROPYLENE FORMULATIONS The following table describes the base formulation:. ... The above procedures for compounding a polypropylene formulation and for making a mono-axially oriented film were followed. The ... The above procedures for compounding a polypropylene formulation and for making a mono-axially oriented film were followed ...
Benzylidene compounds are alkene derivatives of benzene. They are primarily divided into two groups: Styrenes (one benzene) ... Dibenzylideneacetone Aurone Benzylidene Compounds at the US National Library of Medicine Medical Subject Headings (MeSH). ... 6-O-benzylidene-glucopyranose is a glucose molecule whose 4- and 6-OH groups are protected by being bound to a benzylic carbon ... Stilbenes (two benzenes) Benzylidene is also used to describe a type of protecting group in synthetic organic chemistry of the ...
This project is supported by the Canadian Institutes of Health Research (award #111062), Alberta Innovates - Health Solutions, and by The Metabolomics Innovation Centre (TMIC), a nationally-funded research and core facility that supports a wide range of cutting-edge metabolomic studies. TMIC is funded by Genome Alberta, Genome British Columbia, and Genome Canada, a not-for-profit organization that is leading Canadas national genomics strategy with funding from the federal government. Maintenance, support, and commercial licensing is provided by OMx Personal Health Analytics, Inc. Designed by Educe Design & Innovation Inc. ...
Benzylidene Compounds / pharmacology*. Carcinoma, Hepatocellular / drug therapy*, metabolism, pathology. Cell Line, Tumor. Cell ... 0/3,5-bis(2-fluorobenzylidene)piperidin-4-one; 0/Antineoplastic Agents; 0/Benzylidene Compounds; 0/HIF1A protein, human; 0/ ... Phenylurea Compounds / pharmacology, therapeutic use*. Piperidones / pharmacology*. Treatment Outcome. Von Hippel-Lindau Tumor ... Hypoxia-Inducible Factor 1, alpha Subunit; 0/NF-kappa B; 0/Phenylurea Compounds; 0/Piperidones; 0/sorafenib; 25X51I8RD4/ ...
... anabaseine compounds containing a benzylidene substitution at the 3′ position; ANOVA, analysis of variance; GR65630, 3-(5- ... No partial agonism was observed with any of these compounds (Fig. 2A). Antagonistic actions of the BA compounds (0.25-50 μM) ... none of the BA compounds possessed partial agonist activity. BA compounds antagonized 1.5 μM 5-HT-mediated (EC50) responses in ... A, the benzylidene-anabaseine structure is shown. Substitutions with hydroxy (OH) or methoxy (OCH3) were made at the R1 and R2 ...
The present invention provides mercapto-imidazolyl compounds, and the acid addition salts and metal salt complexes thereof; a ... Intermediate compounds useful in the preparation of fungicidal compositions containing (benzylidene)-azolylmethyclycloalkane. ... To produce a suitable preparation of active compound, 1 part by weight of active compound is mixed with the stated amounts of ... To produce a suitable preparation of active compound, 1 part by weight of active compound is mixed with the stated amounts of ...
Categories: Benzylidene Compounds Image Types: Photo, Illustrations, Video, Color, Black&White, PublicDomain, ...
28, 29) and KNK437 (a benzylidene lactam compound; ref. 30). Westerheide et al. ( 5) recently identified triptolide, a ... Yokota S, Kitahara M, Nagata K. Benzylidene lactam compound, KNK437, a novel inhibitor of acquisition of thermotolerance and ...
Benzylidene-heptyl-amine , C14H21N , CID 525555 - structure, chemical names, physical and chemical properties, classification, ...
The effect of benzylidene-quinuclidine compounds on α7 and α3β4 nAChR subtypes. Concentration-response curves for α7-expressing ... Another possibility is that the benzylidine motif does not apply to the Z-isomers. Instead, in the QNZ compounds, the phenyl ... The only compounds that produced detectable activation of muscle-type nAChRs were the non-α7-selective compounds, QN, TMA, and ... Circled compounds are α7-selective. Compounds in filled gray circles had no significant agonist activity when tested at 300 ...
Benzylidene lactam compound, KNK437, a novel inhibitor of acquisition of thermotolerance and heat shock protein induction in ... Preventive effect of ebselen on acute gastric mucosal lesion development in rats treated with compound 48/80 KOBAYASHI T ...
Benzylidene Lactam Compound, KNK437, a Novel Inhibitor of Acquisition of Thermotolerance and Heat Shock Protein Induction in ...
The initial lead compound was prepared as a homologue of the 3-benzylidene-1,3-dihydro-2H-indol-2-one class of kinase inhibitor ... A semiautomated method of ligand docking was used to select compounds for synthesis, and a number of compounds with low ... Compounds in this series inhibited CDK2 with a potency approximately 10-fold greater than that for CDK1. Members of this class ... Two closely related classes of oxindole-based compounds, 1H-indole-2,3-dione 3-phenylhydrazones and 3-(anilinomethylene)-1,3- ...
The initial lead compound was prepared as a homologue of the 3-benzylidene-1,3-dihydro-2H-indol-2-one class of kinase inhibitor ... A semiautomated method of ligand docking was used to select compounds for synthesis, and a number of compounds with low ... Compounds in this series inhibited CDK2 with a potency approximately 10-fold greater than that for CDK1. Members of this class ... Two closely related classes of oxindole-based compounds, 1H-indole-2,3-dione 3-phenylhydrazones and 3-(anilinomethylene)-1,3- ...
The methodology afforded a range of compounds including (Z)-3-(4-(methylsulfonyl)benzylidene)isobenzofuran-1(3H)-one of ...
Yokota S, Kitahara M, Nagata K: Benzylidene lactam compound, KNK437, a novel inhibitor of acquisition of thermotolerance and ...
7, 1995, entitled "Benzylidene-Z-Indoline Compounds for the Treatment of Disease" by Tang et al. (Lyon & Lyon Docket No. 223/ ... 7, 1995, entitled "Benzylidene-Z-Indoline Compounds for the Treatment of Disease" by Tang et al. (Lyon & Lyon Docket No. 223/ ... 5,330,992), styryl compounds (U.S. Pat. No. 5,217,999), styryl-substituted pyridyl compounds (U.S. Pat. No. 5,302,606), certain ... In general, small molecular weight organic compounds are preferred. Examples of classes of compounds that can be tested for ...
Benzylidene-1,3-thiazolidine-2,4-dione compounds for promoting and/or inducing and/or stimulating the pigmentation of keratin ... A standard can be a known compound or another protein known to be present in a sample, for example. As noted above, the test ...
Benzylidene-1,3-thiazolidine-2,4-dione compounds for promoting and/or inducing and/or stimulating the pigmentation of keratin ... However, in these formulations, melatonin is compounded in its undissolved, or solid, state. For any drug to be absorbed into ... In certain embodiments, the solution is mixed with the particles to provide a flowable powder that can be compounded or ... Melatonin is a ubiquitous natural neurotransmitter-like compound produced primarily by the pineal gland, and is involved in ...
Novel Ruthenium Benzylidene Poly[N-Isopropylacrylamide] Compound and a process for the preparation thereof. Disclosed herein is ... Since the ruthenium benzylidene compounds are recoverable and reusable, the cost of catalytic process comes down significantly ... Novel Ruthenium Benzylidene Poly[N-Isopropylacrylamide] Compound and a process for the preparation thereof ... The compound exhibits stability at wide pH (2.010.0) and temperature (440 °C) range. The process of preparation of the novel ...
2-Methoxy-benzylidene)-3H-indol-2-ol , C16H13NO2 , CID 672251 - structure, chemical names, physical and chemical properties, ...
Benzylidene lactam compound, KNK437, a novel inhibitor of acquisition of thermotolerance and heat shock protein induction in ... we used the benzylidene lactam drug, KNK437, which is a highly potent antagonist of the heat shock signaling pathway (22, 29). ...
... an open-chain active methylene compound as a coupling component; methine dyes such as benzylidene dyes and monomethine oxonol ... 15162, and those compounds which are included by the formula of representative compounds and compound examples described in ... An organic fluorine-containing compound may be used in place of the surfactant. Such organic fluorine-containing compounds are ... and fluorine-containing compounds, silicone compounds and chelating agents represented by EDTA may be used as defoaming agents ...
Yokota S, Kitahara M, Nagata K. Benzylidene lactam compound, KNK437, a novel inhibitor of acquisition of thermotolerance and ... In this study, we investigated the effects of a Hsp inhibitor, N-formyl-3,4-methylenedioxy-benzylidene-γ-butyrolactam (KNK437 ... Vascular endothelial growth factor (VEGF) 165 and N-formyl-3,4-methylenedioxy-benzylidene-γ-butyrolactam (a KNK437, Hsp70 ...
... a compound of Formula I: wherein R,sub,1 ,/sub,to R,sub,5 ,/sub,and X,s ... Disclosed are compounds which are nuclear receptor modulators that can act as antagonists to the androgen receptor, for example ... Pati, Hari N., et al., "1,3-DiaryI-2-propenones and 2-Benzylidene-1,3-indandiones: A Quest for Compounds Displaying Greater ... 6. The method of claim 1, wherein the compound is 7. The method of claim 2, wherein the compound is one of the following: 8. ...
  • A semiautomated method of ligand docking was used to select compounds for synthesis, and a number of compounds with low nanomolar inhibitory activity versus CDK2 were identified. (rcsb.org)
  • The present invention discloses a novel metal free process for the regioselective synthesis of α-substituted carbonyl compounds of formula I from alkene, X is selected from the following compounds (A, B). (sumobrain.com)
  • As a research on thiosemicarbazones, the synthesis and crystal structure of a new Schiff base compound derived from thiosemicarbazide and 3-cyanobenzaldehyde has been presented in this article. (pubmedcentralcanada.ca)
  • N-Benzyl-1,3:4,6-di-O-benzylidene-2,5-dideoxy-2,5-imino-L-iditol (cas# 1144513-20-1) is a compound useful in organic synthesis. (trc-canada.com)
  • 2-Acetamido-4,6-O-benzylidene-N-(tert-butoxycarbonyl)-1,2,5-trideoxy-1,5-imino-D-glucitol (cas# 1221795-90-9 ) is a compound useful in organic synthesis. (trc-canada.com)
  • Benzyl 2-Acetamido-4,6-O-benzylidene-3-O-(2,3,4,6-tetra-O-acetyl-β-D-galactopyranosyl-2-deoxy-α-D-glucopyranoside (cas# 67313-30-8) is a compound useful in organic synthesis. (trc-canada.com)
  • Ahsan MJ, Khalilullah H, Yasmin S, Jadav SS, Stables JP, Govindasamy J (2013) Synthesis and anticonvulsant evaluation of 2-(substituted benzylidene/ethylidene)-N-(substituted phenyl)hydrazinecarboxamide analogues. (springer.com)
  • A suitable strategy for the synthesis of a target compound was mostly found on the basis of the intuition and experience of the acting chemists, i.e., the planning of a synthesis of a complex organic molecule was considered as an art form. (chempedia.info)
  • The retrosynthetic analysis of a target compound is a systematic approach in developing a synthesis plan starting with the target structure and working backward to available starting materials. (chempedia.info)
  • In 2015, Engle, Houk, Grubbs, and coworkers developed a model that could rationalize initiation rates of ruthenium olefin metathesis catalysts with chelated benzylidenes, using a combination of organometallic synthesis, reaction kinetics, NMR spectroscopy, X-ray crystallography, and DFT calculations. (wikipedia.org)
  • Ewan achieved the synthesis of this side-product and characterized it as the 5-benzylidene-4-hydroxy-3-phenylfuran-2(5H)-one. (wikipedia.org)
  • These building blocks have been employed in the asymmetric synthesis of numerous biologically active compounds. (wikipedia.org)
  • Recent synthetic developments in a powerful imino Diels-Alder reaction (Povarov reaction): application to the synthesis of N-polyheterocycles and related alkaloids Vladimir V. Kouznetsov Tetrahedron 65 (2009) 2721-2750 doi:10.1016/j.tet.2008.12.059 Unprecedented regio and stereocontrol in Povarov reaction of benzylidene-(3-nitrophenyl)amine Paul J. Stevenson and Isla Graham Arkivoc AM-717D 2003. (wikipedia.org)
  • These approaches can be used to give ligands of differing symmetries, with the direct synthesis route giving homochiral ligands with C3 rotational symmetry and the modular approach typically being used to give asymmetric compounds (C1 symmetry), which are either heterochiral or possess a mix of both chiral and achiral groups. (wikipedia.org)
  • The present study tested the hypothesis that mouse and human 5-hydroxytryptamine 3A (5-HT 3A ) receptors may be differentially modulated by benzylidene analogs of anabaseine (BA) and that these analogs may be useful in assessing residues involved in receptor gating. (aspetjournals.org)
  • The benzylidene anabaseine analogs have also been useful as molecular probes of the ligand binding domains of the α7 nicotinic receptor and 5-HT 3A receptor. (aspetjournals.org)
  • We have shown previously that the benzylidene group of 3-2,4, dimethoxy-benzylidene anabaseine (GTS-21) converts anabaseine into an α7-selective agonist. (aspetjournals.org)
  • Computational studies of benzylidene anabaseine interactions with alpha7 nAChR and acetylcholine binding proteins: application to the design of novel alpha7 selective ligands, a poster presentation scheduled for Wednesday, November 16 at 8:00 a. (thefreedictionary.com)
  • Two closely related classes of oxindole-based compounds, 1H-indole-2,3-dione 3-phenylhydrazones and 3-(anilinomethylene)-1,3-dihydro-2H-indol-2-ones, were shown to potently inhibit cyclin-dependent kinase 2 (CDK2). (rcsb.org)
  • This invention is based on the unexpected discovery that a group of piperazinedione compounds effectively inhibit tyrosine kinase and suppress cancer growth. (patentgenius.com)
  • The present invention relates to novel compounds selected from 2-aminoaryloxazoles that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic and degenerative disorders. (google.com)
  • We here explored the phenotypic response of colon cancer cells to b-AP15, a bis-benzylidine piperidone previously shown to inhibit the proteasome deubiquitinases (DUBs) USP14 and UCHL5. (diva-portal.org)
  • Previously, we identified a collection of 10-benzylidene-10H-anthracen-9-ones that effectively inhibit AR transcriptional activity, induce AR degradation and display some ability to block recruitment of hormones to the receptor. (nih.gov)
  • Anticancer and antioxidant activity of synthetic chalcones and related compounds," Cancer Letters, vol. 97, No. 1, pp. 33-37 (Oct. 20, 1995). (freepatentsonline.com)
  • The anticancer activity (IC 50 = µmol/mL) of the synthesized compounds was determined against human colorectal carcinoma (HCT116) cancer cell line by Sulforhodamine B (SRB) assay. (pubmedcentralcanada.ca)
  • The compounds were also assessed for their anticancer activity exhibited using the SRB assay and were found to elicit antiproliferative activity against MCF7 breast cancer cell line, which was comparable to the standard drug. (springer.com)
  • The anticancer screening results revealed that compounds, 12 , 21 , 22 and 29 to show the highest activity against MCF7 and their IC 50 values were more potent than 5-fluorouracil. (springer.com)
  • The synthesized compounds were screened for their in vitro antimicrobial potential against Gram (positive and negative) bacterial and fungal strains by tube dilution technique. (biomedcentral.com)
  • The synthesized compounds were screened for analgesic (100 and 200 mg/kg), antiinflammatory (200 and 400 mg/kg), antibacterial ( Bacillus subtilis, Bacillus cereus, Staphylococcus epidermidis, Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas aeruginosa and Escherichia coli ) and antifungal ( Candida albicans and Aspergillus niger ) activities. (ijpsonline.com)
  • The synthesized compounds were screened for analgesic activity by chemical writhing and Eddy's hot plate method, antiinflammatory activity by paw edema method, anti-bacterial and anti-fungal activities. (ijpsonline.com)
  • The synthesized compounds were screened for their antimicrobial and antiproliferative activities. (springer.com)
  • The aromatic substitution reactions are not limited to azobenzene and benzylidene but are even more facile with N,N-dimethylbenzylamine [13, (thefreedictionary.com)
  • The target compounds were synthesized from diethyl succinate and benzaldehyde or 4-fluorobenzaldehyde by four-step reactions. (bvsalud.org)
  • Reactions of 1,3-diethyl-2-thiobarbituric acid with aldehydes: formation of arylbis(1,3-diethyl-2-thiobarbitur-5-yl)methanes and crystallographic evidence for ground state polarisation in 1,3-diethyl-5-[4-(dimethylamino)benzylidene]-2-thiobarbituric acid, Journal of the Chemical Society, Perkins Transactions 1, Chemical Society, pp. 2483-2488 (1999). (freepatentsonline.com)
  • The catalytic constants for the reactions catalysed by acetic and formic acids are similar to those of the analogously catalysed hydrolyses of OO-(4-carboxybenzylidene) catechol, but the catalytic constant for the spontaneous reaction is ca. 30 times greater than that for spontaneous hydrolysis of the latter compound. (hud.ac.uk)
  • 5. Changcheng Jing, Dong Xing, Yu Qian, Taoda Shi, Yun Zhao, and Wenhao Hu*, Diversity-Oriented Three-Component Reactions of Diazo Compounds with Anilines and 4-Oxo-Enoates. (sysu.edu.cn)
  • 12. Wenhao Hu*, Xinfang Xu, Jing Zhou, Wei-Jun Liu, Haoxi Huang, Juan Hu, Liping Yang, and Liu-Zhu Gong*, Cooperative Catalysis with Chiral Brønsted Acid-Rh2(OAc)4: Highly Enantioselective Three-Component Reactions of Diazo Compounds with Alcohols and Imines, J. Am. Chem. (sysu.edu.cn)
  • Side reactions include the formation of α-bromoketones and dibromo compounds. (wikipedia.org)
  • Compounds 11 and 12, in a concentration-dependent manner, inhibited EGF receptor tyrosine kinase activity. (amrita.edu)
  • We also studied the three-dimensional structures (folding) of short peptides having the amino acid sequence of the IGF-1R tyrosine domain, including the tyrosine residues at positions 1131, 1135, and 1136, constructed by the computer, to find compounds having the ability to mimic the tyrosine residues and thereby interfere with their phosphorylation (substrate phosphorylation). (aacrjournals.org)
  • We are a company that believes in using state-of-the-art technology and, therefore, we use technologically advance machinery and other tools to offer our customers a wide range of additives, intermediates, chemicals and their compounds. (tradeindia.com)
  • About nine (E)-(2,5-dinitrophenyl)-2-(substituted benzylidene)hydrazines have been synthesized by hydroxy apatite catalyzed condensation of 2,4-dinitrophenyl hydrazine and substituted benzaldehydes under microwave irradiation conditions. (infona.pl)
  • In the present study, a series of nine number of ( E )-1-benzylidene-2-(4-chlorophenyl) hydrazine compounds have been synthesized by condensation reaction of meta and para substituted benzaldehydes with 4-chlorophenylhydrazine using acetic acid catalyst. (scipress.com)
  • The antimicrobial activities of all the synthesized ( E )-1-benzylidene-2-(4-chlorophenyl) hydrazine compounds have been studied using Bauer-Kirby method. (scipress.com)
  • These hydroxyl groups were assigned, one each, to the last five carbon atoms, because geminal hydroxyl groups are normally unstable relative to the carbonyl compound formed by loss of water. (msu.edu)
  • class of compounds, the sulphenyl bromides 3, in quantitative yield. (docme.ru)
  • By studying a benzylidene-type push-pull chromophore bearing a 5-carboxy- BDMI electron-acceptor and 4-(dimethylamino)aniline donor fragment, we demonstrate that this class of compounds can show unusual response to the polarity of the surrounding medium. (rsc.org)
  • The activity of the these compound was the most probably due to presence of hydroxyl group at third position of aniline ring in 6c, benzyl group in 3d and two alkyl groups at third and fifth position of aniline ring in 6a along with benzyl group attached to nitrogen of sulfonamide. (thefreedictionary.com)
  • The compound exhibits a combination of catalytic, antibacterial, anti-fouling and adsorptive properties. (clri.org)
  • Recently we have developed a panel of small molecular compounds targeting a non-catalytic site of PP1. (biomedcentral.com)
  • As with other Grubbs-type catalysts with modified chelating benzylidenes, after one catalytic turnover, the chelate is no longer associated with the propagating catalyst, meaning that the initiate rate, the rate of o-alkoxystyrene rechelation, and the rates of various catalyst decomposition events are the factors that differ between the Zhan catalysts and the parent Hoveyda-Grubbs catalysts. (wikipedia.org)
  • 2) involved the incorporation of a healing agent in an epoxy matrix: microencapsulated monomer dicyclopentadiene (DCPD) and wax microspheres containing Grubbs' catalyst, bis(-tricyclohexylphosphine) benzylidene ruthenium (IV) dichloride. (thefreedictionary.com)
  • All synthesized chalcone compounds could be used to visualize hH 3 R proteins in stably transfected HEK-293 cells using confocal laser scanning fluorescence microscopy. (frontiersin.org)
  • In this series, compound 10 exhibited significant antimicrobial activity against B . subtilis and S . aureus with MIC = 4.2 × 10 −2 µM/ml, compound 15 showed significant activity against K . pneumonia with MIC = 2.60 × 10 −2 µM/ml and compound 4 displayed potent antibacterial activity against E . coli with MIC = 4.5 × 10 −2 µM/ml. (biomedcentral.com)
  • The synthesized benzimidazole compounds were evaluated for their antimicrobial activity using the tube dilution method and were found to exhibit good antimicrobial potential against selected Gram negative and positive bacterial and fungal species. (springer.com)
  • The reaction mixture was cooled for a while and solid separated was filtered and recrystallised from ethanol (99%) yield the title compounds (1-5). (ijpsonline.com)
  • In the first step, a dirhodium catalyst effects diazo decomposition from silyl enol ether diazo compound to yield a donor/acceptor cyclopropene. (wikipedia.org)
  • and (v) granule count, to determine whether the candidate compound is a modulator of heat shock protein (HSP) expression or a modulator of heat shock transcription factor (HSF) expression. (patentsencyclopedia.com)
  • Ecamsule (USAN, trade name Mexoryl SX, INCI terephthalylidene dicamphor sulfonic acid) is an organic compound which is added to many sunscreens to filter out UVA rays. (wikipedia.org)
  • Pulvinone, an organic compound belonging to the esters, lactones, alcohols and butenolides classes, is a yellow crystalline solid. (wikipedia.org)
  • The synthesized compounds were evaluated on the basis of spectral analysis: IR, NMR and Mass and elemental analyses which were in full agreement with their proposed molecular structures. (springer.com)
  • Diene polymers or copolymers having improved balance between raw polymer viscosity and mixed compound viscosity, useful in tire tread compositions having highly balanced wet traction, rolling resistance, and traction in ice and snow, and fracture properties in the cured and white carbon reinforced states are provided. (google.com)
  • To maintain simplicity we neglect elastic effects and the variations of compound viscosity with mixing, and focus on the simulation of the flow corresponding to a generalized Newtonian fluid. (chempedia.info)
  • This places limitations on the NLO applications of the studied compound and its structural analogues, as the surrounding medium (solvent of polymer matrix) with the lowest possible polarity needs to be used to maximize their NLO efficiency. (rsc.org)