Compounds containing the PhCH= radical.
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.
The largest country in North America, comprising 10 provinces and three territories. Its capital is Ottawa.
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)
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)
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.
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.
A fungistatic compound that is widely used as a food preservative. It is conjugated to GLYCINE in the liver and excreted as hippuric acid.
Derivatives of BENZOIC ACID. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain the carboxybenzene structure.
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.
Substances capable of inhibiting, retarding or arresting the process of fermentation, acidification or other deterioration of foods.
An expectorant that also has some muscle relaxing action. It is used in many cough preparations.
Detailed account or statement or formal record of data resulting from empirical inquiry.
A loose confederation of computer communication networks around the world. The networks that make up the Internet are connected through several backbone networks. The Internet grew out of the US Government ARPAnet project and was designed to facilitate information exchange.
The portion of an interactive computer program that issues messages to and receives commands from a user.
Databases containing information about PROTEINS such as AMINO ACID SEQUENCE; PROTEIN CONFORMATION; and other properties.
Sequential operating programs and data which instruct the functioning of a digital computer.
The addition of descriptive information about the function or structure of a molecular sequence to its MOLECULAR SEQUENCE DATA record.
Linear POLYPEPTIDES that are synthesized on RIBOSOMES and may be further modified, crosslinked, cleaved, or assembled into complex proteins with several subunits. The specific sequence of AMINO ACIDS determines the shape the polypeptide will take, during PROTEIN FOLDING, and the function of the protein.
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.
A dipolar ionic buffer.
Aminobenzoate derivatives that contain an amino group attached to carbon number 3 or 5 of the benzene ring structure.
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)
A white, crystalline powder that is commonly used as a pH buffering agent, an electrolyte replenisher, systemic alkalizer and in topical cleansing solutions.
Benzoic acids, salts, or esters that contain an amino group attached to carbon number 2 or 6 of the benzene ring structure.
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.
Exclusive legal rights or privileges applied to inventions, plants, etc.
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)
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)
A novel composition, device, or process, independently conceived de novo or derived from a pre-existing model.
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)
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.
A trace element with the atomic symbol Ni, atomic number 28, and atomic weight 58.69. It is a cofactor of the enzyme UREASE.
A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.
Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.
A class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins.
Agents that induce NARCOSIS. Narcotics include agents that cause somnolence or induced sleep (STUPOR); natural or synthetic derivatives of OPIUM or MORPHINE or any substance that has such effects. They are potent inducers of ANALGESIA and OPIOID-RELATED DISORDERS.
An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.
Compounds with activity like OPIATE ALKALOIDS, acting at OPIOID RECEPTORS. Properties include induction of ANALGESIA or NARCOSIS.
The principal alkaloid in opium and the prototype opiate analgesic and narcotic. Morphine has widespread effects in the central nervous system and on smooth muscle.
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.
Ducts that collect PANCREATIC JUICE from the PANCREAS and supply it to the DUODENUM.
Carcinoma that arises from the PANCREATIC DUCTS. It accounts for the majority of cancers derived from the PANCREAS.
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.
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.
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).
Silicon polymers that contain alternate silicon and oxygen atoms in linear or cyclic molecular structures.
Substances intended to be applied to the human body for cleansing, beautifying, promoting attractiveness, or altering the appearance without affecting the body's structure or functions. Included in this definition are skin creams, lotions, perfumes, lipsticks, fingernail polishes, eye and facial makeup preparations, permanent waves, hair colors, toothpastes, and deodorants, as well as any material intended for use as a component of a cosmetic product. (U.S. Food & Drug Administration Center for Food Safety & Applied Nutrition Office of Cosmetics Fact Sheet (web page) Feb 1995)
A broad family of synthetic organosiloxane polymers containing a repeating silicon-oxygen backbone with organic side groups attached via carbon-silicon bonds. Depending on their structure, they are classified as liquids, gels, and elastomers. (From Merck Index, 12th ed)
Antineoplastic agent that is also used as a veterinary anesthetic. It has also been used as an intermediate in organic synthesis. Urethane is suspected to be a carcinogen.
Organic siloxanes which are polymerized to the oily stage. The oils have low surface tension and density less than 1. They are used in industrial applications and in the treatment of retinal detachment, complicated by proliferative vitreoretinopathy.
Polymers of silicone that are formed by crosslinking and treatment with amorphous silica to increase strength. They have properties similar to vulcanized natural rubber, in that they stretch under tension, retract rapidly, and fully recover to their original dimensions upon release. They are used in the encapsulation of surgical membranes and implants.
Procedures for the improvement or enhancement of the appearance of the visible parts of the body.

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] strongly as well as succinate dehydrogenase [EC],.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
Benzylidene camphor sulfonic acid, Benzylidene camphor sulfonic acid supplier, Benzylidene camphor sulfonic acid distributor, CAS 56039-58-8, Benzylidene camphor sulfonic acid manufacturer, Benzylidene camphor sulfonic acid wholesale
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.
Table_1_Role of Neutral Sphingomyelinase-2 (NSM 2) in the Control of T Cell Plasma Membrane Lipid Composition and Cholesterol Homeostasis.DOCX
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.
TY - JOUR. T1 - κ And δ opioid receptor stimulation affects cardiac myocyte function and Ca2+ release from an intracellular pool in myocytes and neurons. AU - Ventura, C.. AU - Spurgeon, H.. AU - Lakatta, E. G.. AU - Guarnieri, C.. AU - Capogrossi, M. C.. PY - 1992. Y1 - 1992. N2 - We investigated the effects of μ, δ, and κ opioid receptor stimulation on the contractile properties and cytosolic Ca2+ (Ca(i)) of adult rat left ventricular myocytes. Cells were field-stimulated at 1 Hz in 1.5 mM bathing Ca2+ at 23°C. The μ-agonist [D-Ala2,N-Me-Phe4,Gly5-ol]-enkephalin (10-5 M) had no effect on the twitch. The δ-agonists methionine enkephalin and leucine enkephalin (10-10 to 10-6 M) and the κ-agonist (trans-(dl)- 3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclo-hexyl]-benzeneacetamide) methanesulfonate hydrate (U-50,488H; 10-7 to 2x10-5 M) had a concentration-dependent negative inotropic action. The sustained decrease in twitch amplitude due to U-50,488H was preceded by a transient increase ...
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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
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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 ...
Fingerprint Dive into the research topics of NCI in vitro and in silico anticancer screen, cell cycle pertubation and apoptosis-inducing potential of new acylated, benzylidene and isopropylidene derivatives of andrographolide. Together they form a unique fingerprint. ...
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,
TY - JOUR. T1 - In vitro and in vivo imaging of nitroxyl with copper fluorescent probe in living cells and zebrafish. AU - Palanisamy, Sathyadevi. AU - Wang, Yu Liang. AU - Chen, Yu Jen. AU - Chen, Chiao Yun. AU - Tsai, Fu Te. AU - Liaw, Wen Feng. AU - Wang, Yun-Ming. PY - 2018/10/6. Y1 - 2018/10/6. N2 - Nitroxyl (HNO) plays a critical role in many physiological processes which includes vasorelaxation in heart failure, neuroregulation, and myocardial contractility. Powerful imaging tools are required to obtain information for understanding the mechanisms involved in these in vivo processes. In order to develop a rapid and high sensitive probe for HNO detection in living cells and the zebrafish model organism, 2-((2-(benzothiazole-2yl)benzylidene) amino)benzoic acid (AbTCA) as a ligand, and its corresponding copper(II) complex Cu(II)-AbTCA were synthesized. The reaction results of Cu(II)-AbTCA with Angelis salt showed that Cu(II)-AbTCA could detect HNO quantitatively in a range of 40-360μM with ...
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 ...
The two figures below are plots of representative Spinach and FAP fluorescence over time (from two replicates). The figures compare the fluorescence of three new T7Lac promoters with the wild-type T7Lac promoter, when either 3,5-difluoro-4-hydroxybenzylidene imidazolinone (DFHBI) or Malachite Green (MG) was added. DFHBI is a specific fluorogen that binds to Spinach and MG is a specific fluorogen that binds to FAP. Therefore, we assume that there is a positive correlation between fluorescence values and the amount of either RNA and proteins in bacteria. All fluorescence values are normalized by the corresponding OD600 readings. Please refer to the Time-Lapse protocol in the Protocols page for the full experimental details ...
The two figures below are plots of representative Spinach and FAP fluorescence over time (from two replicates). The figures compare the fluorescence of three new T7Lac promoters with the wild-type T7Lac promoter, when either 3,5-difluoro-4-hydroxybenzylidene imidazolinone (DFHBI) or Malachite Green (MG) was added. DFHBI is a specific fluorogen that binds to Spinach and MG is a specific fluorogen that binds to FAP. Therefore, we assume that there is a positive correlation between fluorescence values and the amount of either RNA and proteins in bacteria. All fluorescence values are normalized by the corresponding OD600 readings. Please refer to the Time-Lapse protocol in the Protocols page for the full experimental details ...
[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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The intramolecular cyclizations of the 3-alkyne-1,2-diols and the 1-amino-3-alkyn-2-ols with a low catalyst loading (0.05-0.5 mol… Expand ...
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 ...
TY - JOUR. T1 - Trifluoromethanesulfonic acid-catalyzed tandem semi-pinacol rearrangement/alkyne-aldehyde metathesis reaction of arylpropagylsulfonamide- tethered 2,3-epoxycyclohexan-1-ols to spiropiperidines. AU - Lin, Ming Nan. AU - Wu, Shih Hui. AU - Yeh, Ming-Chang P.. PY - 2011/12/1. Y1 - 2011/12/1. N2 - A simple and efficient trifluoromethanesulfonic acid-catalyzed cycloisomerization of arylpropagylsulfonamide-tethered 2,3-epoxycyclohexan-1-ols is described. The cyclization proceeds via tandem semi-pinacol rearrangement/alkyne-aldehyde metathesis to afford spiropiperidines under mild reaction conditions.. AB - A simple and efficient trifluoromethanesulfonic acid-catalyzed cycloisomerization of arylpropagylsulfonamide-tethered 2,3-epoxycyclohexan-1-ols is described. The cyclization proceeds via tandem semi-pinacol rearrangement/alkyne-aldehyde metathesis to afford spiropiperidines under mild reaction conditions.. KW - alkyne/aldehyde metathesis. KW - semi-pinacol rearrangement. KW - ...
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 ...
Two novel complexes for Zn2+ and VO2+ ions, were prepared from tridentate dibasic chelating Schiff base ligand. 1-((3,5-di-tert-butyl-2-hydroxybenzylidene)amino)naphthalen-2-ol-5‑sodium sulfonate (DSHN), was the ligand used in this study. Alternative spectral tools were applied to elucidate structural composition of new compounds. Also, geometry optimization for all synthesizes was conducted by Gaussian09 program via DFT method, to obtain optimal structures and essential parameters. Moreover, the biochemical behavior for all synthesizes, was explored based on tested reactivity against various microbial strains and cancer cells (HCT-116, MCF-7, and HepG-2). The two complexes exhibited interestingly anti-proliferative potential against human cancer cell lines. The antioxidant behavior of the two complexes was studied by DPPH and SOD assays. Particularly, Zn(II) and VO(II) complexes presented more enhanced antimicrobial and anticancer features compared to the free ligand (DSHN), with superiority ...
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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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.
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... are, formally speaking, derivatives of benzylidene, although few are prepared from the carbene. ... 6-O-benzylidene-glucopyranose is a glucose derivative. Benzylidene is an archaic term for compounds of the type PhCHX2 and PhCH ... Benzylidene+Compounds at the US National Library of Medicine Medical Subject Headings (MeSH) v t e. ... Benzal chloride, PhCHCl2, is alternatively named benzylidene chloride. Benzylidene is the molecule C6H5CH. It is a triplet ...
... s are used as protecting groups in glycochemistry. These compounds can also be oxidized to carboxylic acids ... In organic chemistry, a benzylidene acetal is the functional group with the structural formula C6H5CH(OR)2 (R = alkyl, aryl). ... S. Hanessian (1987). "6-Bromo-6-deoxy Hexose Derivatives By Ring Opening Of Benzylidene Acetals With N-bromosuccinimide: Methyl ... Banerjee, Amit; Senthilkumar, Soundararasu; Baskaran, Sundarababu (2015-12-07). "Benzylidene Acetal Protecting Group as ...
3-benzylidene camphor (3BC) Benzylidene camphor sulfonic acid (BCSA) 4-methylbenzylidene camphor (4-MBC) Polyacrylamidomethyl ... UV filters are compounds, mixtures, or materials that block or absorb ultraviolet (UV) light. One of the major applications of ... The 4-methyl-benzylidene camphor was detected in the muscle tissue of trout in Swiss and German waters, while traces of ... UV classifications include UVA (320-400 nm), UVB (290-320 nm) and UVC (200-280 nm). UV-absorbing compounds are used not only in ...
... 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 ...
An aurone is a heterocyclic chemical compound which is a type of flavonoid. There are two isomers of the molecule, with (E)- ... 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. Benzaldehyde is commonly employed to ... 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 ... Bromination of unsaturated compounds with N-bromoacetamide, a contribution to the theory of the course of chemical processes]. ...
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, ...
Although many compounds contain an acetal functional group, at least two acetal compounds are called "acetal" for short: ... Benzylidene acetal, a protecting group Dimethoxymethane, a solvent, a.k.a. methylal, a.k.a. formal [ambiguous] Dioxolane ... Various specific carbonyl compounds have special names for their acetal forms. For example, an acetal formed from formaldehyde ... 1,1-Diethoxyethane (acetaldehyde diethyl acetal), sometimes called simply "acetal", is an important flavouring compound in ...
... , 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 ...
... these compounds are also chiral, and are referred to as S-chiral sulfinamides. Sulfinamides are amides of sulfinic acid (RS(O) ... BENZYLIDENE)-p-TOLUENESULFINAMIDE". Organic Syntheses. 77: 50.CS1 maint: multiple names: authors list (link); Collective Volume ...
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 (21): 7037-7039 ... "Asymmetric Synthesis of β-Amino Carbonyl Compounds with N-Sulfinyl β-Amino Weinreb Amides". Journal of Organic Chemistry. 70 (6 ...
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. ...
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) ...
... (also known as alane or alumane) is an inorganic compound with the formula AlH3. It presents as a white solid ... 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 ...
Because the enolizeable nucleophilic carbonyl compound and the electrophilic carbonyl compound are two different chemicals, the ... Substituted-benzylidene)cycloalkanones and α,α′-bis-(Substituted-alkylidene)cycloalkanones". Molecules. 17: 571-583. doi: ... However, this problem can be avoided if one of the compounds does not contain an α-hydrogen, rendering it non-enolizable. In an ... The reaction between an aldehyde or ketone having an α-hydrogen with an aromatic carbonyl compound lacking an α-hydrogen is ...
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 ...
Benzylidene compounds are, formally speaking, derivatives of benzylidene, although few are prepared from the carbene. ... 6-O-benzylidene-glucopyranose is a glucose derivative. Benzylidene is an archaic term for compounds of the type PhCHX2 and PhCH ... Benzylidene+Compounds at the US National Library of Medicine Medical Subject Headings (MeSH) v t e. ... Benzal chloride, PhCHCl2, is alternatively named benzylidene chloride. Benzylidene is the molecule C6H5CH. It is a triplet ...
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 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. *Central Nervous System Agents. *Chromones. *Compounds used in a research, industrial, or household ...
A tri-benzyl-idene-methane-tantalum compound: some experiences with `inversion twinning. W. P. Schaefer, R. E. Marsh, G. ... 3 + 2)-Dimensional superspace approach to the structure of the stage-2 misfit layer compound (SbS)1.15(TiS2)2. ... Vacancies and electron localization in the incommensurate intergrowth compound (La0.95Se)1.21VSe2. ... Benzene-1,2-di-sulfonate dianion: another compound with meshed cogwheel substituents?. ...
... 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 ...
Benzylidene Compounds / pharmacology* * Cell Division / drug effects * Dose-Response Relationship, Drug * Electrophoresis, ...
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/ ...
0 (Antitrichomonal Agents); 0 (Benzylidene Compounds); 0 (Receptors, Opioid, delta); 129468-28-6 (7-benzylidenenaltrexone); ... Eight compounds, including five flavonoids, were identified with IC50 values ⩽10 M and confirmed in counter screens run in the ... The four mentioned compounds exhibited non-cytotoxic profiles at all of the concentrations assayed, showing a fair ... Nitroimidazoles are compounds having azomycin (2-nitroimidazole) chemical structure and are obtained from Streptomyces strains ...
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, ...
Benzylidene Compounds / pharmacology * Cell Line * Cell Membrane / metabolism * Cyclic AMP / metabolism * Dose-Response ...
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 ...
Previous Patent: Benzylidene-1,3-thiazolidine-2,4-dione compounds for promoting and/or inducing and/or stimulating th.... Next ... or compounds formed by reacting isocyanates with hydroxy-containing compounds, for example: OCN-B+OH-(CH2)x-CH3. or compounds ... The preferred compound is ethylhexyl methoxycinnamate, also referred to as Octoxinate or octyl methoxycinnamate. The compound ... refers to a compound or monomer formed by reacting an isocyanate with hydroxy-substituted compounds, for example: wherein B is ...
... is A cell permeable benzylidene rhodanine compound. MF: C17H11Br2NO2S2, MW: 485.21. Cited in 1 publications ... PRL-3 Inhibitor is a cell-permeable benzylidene rhodanine compound that potently inhibits PRL-3 (hPRL-3), a member of the ... Alternate Names: 1-(2-Bromobenzyloxy)-4-bromo-2-benzylidene rhodanine Application: PRL-3 Inhibitor is a cell permeable ... 4-bromo-2-benzylidene rhodanine showed a significant ability to inhibit PRL-3. -SCBT Publication Review Date published: 2015-04 ...
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 ...
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 ...
... a yellow polyphenol compound, is known to possess antifungal activity for a range of pathogenic fungi. However, the fungicidal ... Benzylidene-carbonyl compounds are active against itraconazole-susceptible and itraconazole-resistant Sporothrix brasiliensis ... Curcumin, a yellow polyphenol compound, is known to possess antifungal activity for a range of pathogenic fungi. However, the ...
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 ...
The (E)-1-benzylidene-2-(3-nitrophenyl)hydrazine compounds with parent (H), 3-Br, 4-Br, 3-Cl, 4-Cl, 4-F, 4-C[H.sub.3] and 4- OC ... The 4-F substituted (E)-1-benzylidene-2-(3-nitrophenyl)hydrazine compound has shown very good antifungal activity against ... 4-F, 4-OC[H.sub.3], 3-N[O.sub.2] and 3-O[C.sub.6][H.sub.5] substituted compounds have shown good activity against A. ... The 4-F substituted compound has shown excellent activity against Enterococcus species and E. ...
Yokota S, Kitahara M, Nagata K: Benzylidene lactam compound, KNK437, a novel inhibitor of acquisition of thermotolerance and ...
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 ...
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). ...
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 ...
  • Benzylidene compounds are, formally speaking, derivatives of benzylidene, although few are prepared from the carbene. (
  • Employing purified protein phosphotyrosine phosphatase, and benzylidene derivatives (tyrphostins: compounds 11 and 12) that selectively inhibit EGF receptor protein tyrosine kinase (EGFRK) activity, the role of EGFRK in EGF-mediated stimulation of cardiac adenylyl cyclase was investigated. (
  • In the present study, benzylidene-2,4-thiazolidinedione derivatives (compounds 2-5) were synthesized and screened against cancer cell lines and the genotoxicity and cytotoxicity of the most active compound (5) was investigated on normal and lung cancer cell line. (
  • Some of the benzylidene and 2-benzyl derivatives with free rotation at C2 position exhibited potential cytotoxicities against various human cancer cell lines. (
  • The invention relates to new chemical compounds, particularly to derivatives of 2-aminoindole that exhibit hepatoprotective activity and can find application in medical practice. (
  • Benzylidene derivative of chloroaldehyde was prepared by Vilsmeier reaction of 2-benzylidenecyclohexanone derivatives, which were obtained from the condensation of various aromatic aldehydes with cyclohexanone. (
  • Results: Benzylidene derivatives of 1,2,3,4-Tetrahydro-Dibenzo[b,f][1,4]Oxazepine 6a-g exhibited promising antiproliferative activity with GI50 values in the micromolar range. (
  • This encouraged the design, synthesis and evaluation of non-xanthine derivatives, generally amino-substituted heterocyclic compounds. (
  • 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. (
  • 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). (
  • These compounds can also be oxidized to carboxylic acids in order to open important biological molecules, such as glycosaminoglycans, to other routes of synthesis. (
  • Chapter 3 describes the synthesis of a series of ruthenium benzylidenes containing N-heterocyclic carbene ligands. (
  • 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. (
  • Alsaygh, A. , Al-Humaidi, J. and Al-Najjar, I. (2014) Synthesis of Some New Pyridine-2-yl-Benzylidene-Imines. (
  • 13] Al-Douh, M.H., Al-Fatlawy, A.A. and Abid, O.H. (2004) Synthesis and Characterization of Some 2-(N-Benzoyl- N-Pyrid-2-yl Amino-benzyl)Aminobarbituric Acids via N-Benzylidene Pyridine-2-Amines. (
  • 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. (
  • In conclusion, the current study involved the synthesis, characterisation and evaluation of novel 5-substituted 2-benzylidene-1-tetralone analogues to understand the importance of structural modifications to ring A and B of the aurone and 2-benzylidene-1-tetralone scaffold in gaining or even losing A1 and/or A2A AR affinity. (
  • 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. (
  • 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. (
  • 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. (
  • Synthesis, HIV-1 RT inhibitory, antibacterial, antifungal and binding mode studies of some novel N-substituted 5-benzylidine-2,4-thiazolidinediones. (
  • For example, 4,6-O-benzylidene-glucopyranose is a glucose derivative. (
  • The 6-Hydroxy-2-oxo-1,2-dihydropyridine-4-carboxylic acid (6) chemical compound and its derivative, 3-Benzylidene-2,6-dioxo-1,2,3,6-tetrahydropyridine-4-carboxylic acid (13), showed enzyme inhibition constants in the submicromolar range. (
  • The disclosed subject matter provides N-substituted hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. (
  • The isomers were separated by way of the benzylidene derivative [41 of the cis-compound and were compared by 1R spectroscopy with the same compounds obtained from pyrocatechol by hydrogenation over the same Ni-MgO catalyst. (
  • The valuable properties of "glitazones" initiated us to synthesize N-substituted-5-benzylidene-2,4-TZD derivative. (
  • A logically designed and identified lead compound, fluorinated benzylidene indanone 1 has been extensively evaluated for cancer pharmacology. (
  • 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. (
  • Compounds in filled gray circles had no significant agonist activity when tested at 300 μMon α7, α4β2, or α3β4 receptors (data not shown). (
  • PRL-3 Inhibitor is a cell-permeable benzylidene rhodanine compound that potently inhibits PRL-3 (hPRL-3), a member of the regenerating liver family tyrosine phosphatases. (
  • A cell-permeable ( bis -benzylidene)piperidinone compound that acts as a selective inhibitor against CARM1/PRMT4 arginine methyltransferase activity (IC 50 = 7.1 µM with PABP1 as substrate). (
  • Benzylidene acetal is a protecting group in synthetic organic chemistry of the form PhCH(OR)2. (
  • These include dimers linked at C-4 by either rigid or flexible amines, and monomers possessing either a dimethyl or benzylidene acetal in the A-ring. (
  • In organic chemistry, a benzylidene acetal is the functional group with the structural formula C6H5CH(OR)2 (R = alkyl, aryl). (
  • Thiazolidine-2,4-dione ring system is used as a pharmacophore to build various heterocyclic compounds aimed to interact with biological targets. (
  • Several of these compounds were characterized by X-ray crystallography, and the barriers to benzylidene and N-heterocyclic carbene rotation were determined using [superscript 1]H NMR spectroscopy. (
  • 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. (
  • We have shown previously that the benzylidene group of 3-2,4, dimethoxy-benzylidene anabaseine (GTS-21) converts anabaseine into an α7-selective agonist. (
  • 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. (
  • abstract = "Fluorescent polymers imprinted with various N1-benzylidene pyridine-2-carboxamidrazones were evaluated for their recognition of the original template and cross-reactivity to similar molecules. (
  • 3. The compound of claim 2, wherein Ar.sub.1 is phenyl and Ar.sub.2 is pyridinyl. (
  • The synthesized 1-{[3-(furan-2-yl)-5-phenyl-4,5-dihydro-1,2-oxazol-4-yl]methyl}-4-methyl piperazine compounds were characterized by means of their IR and NMR spectral data. (
  • Two new low-molecular weight compounds - (Z)-4-(4-(dimethylamino)benzylidene)-1-(9-ethyl-9H-carbazol-3-yl)-2-phenyl-1H-imidazol-5(4H)-one and 2-(6-hydroxyhexyl)-6-(pyrrolidin-1-yl)-1H-benzo[de]isoquinoline-1,3(2H)-dione) - with possible application in organic light-emitting devices were synthesized. (
  • It was found that C5-OH substitution on ring A of the benzylidene tetralones in combination with meta (C3')- and/or para (C4')-OH substitution on phenyl ring B of these scaffolds are ideal for A1 and/or A2A AR affinity. (
  • Furthermore, substitution of phenyl ring B of the benzylidene tetralones with a 2-aminopyrimidine ring resulting in moderate to high A2A AR affinity. (
  • A series of novel substituted 2-(5-benzylidene-2,4-dioxothiazolidin-3-yl)-N-(phenyl)propanamides (4-31) have been synthesized and evaluated for their HIV-1 RT inhibitory activity, antibacterial and antifungal activities. (
  • The (E)-1-benzylidene-2-(3-nitrophenyl)hydrazine compounds with parent (H), 3-Br, 4-Br, 3-Cl, 4-Cl, 4-F , 4-C[H.sub.3] and 4- OC[H.sub.3] substituents have shown good activity against Staphylococcus aureus. (
  • 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. (
  • The antimicrobial activities of all the synthesized ( E )-1-benzylidene-2-(4-chlorophenyl) hydrazine compounds have been studied using Bauer-Kirby method. (
  • Chapter 4 describes the preparation of a series of four-coordinate ruthenium benzylidenes that serve as analogues of the 14-electron olefin metathesis intermediate (L)(Cl)[subscript 2]Ru=CHPh. (
  • Known structural analogues of the claimed compounds [1]. (
  • 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. (
  • These compounds are tyrosine kinase inhibitors and can be used to treat cancer. (
  • 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. (
  • The compounds containing halo, alkyl and alkoxyl groups as substituents on the benzylidine ring have been found to be very effective cytotoxic agents. (
  • Structures of the compounds were elucidated using various spectral techniques viz. (
  • α , α′ - bis ( p -Dimethylamino benzylidene)- g -methylcyclohexanone (BMABMC) C 25 H 30 ON 2, has been synthesised and characterised by elemental analysis, spectral data and XRD studies. (
  • Conformations of the structures were assigned on the basis of results of different spectral data.Some of the compounds have shown significant activity.Molecular docking studies showed very good interaction. (
  • Benzylidene is the molecule C6H5CH. (
  • There have been other benzaldehydes used in cancer such as glyco benzylidene extracted from the Japanese fig, (1) but this molecule was so difficult to extract it had to be synthesized. (
  • Scientists have designed another potentially pharmacologically useful compound - GC-24 (4), a second-generation thyromimetic molecule that differs from GC-1 (3) in the 3' position of the second aromatic ring, where a benzyl group substitutes the isopropyl group (Figure 2). (
  • Benzylidene is an archaic term for compounds of the type PhCHX2 and PhCH= substituents (Ph = C6H5). (
  • A series of rhodanine compounds containing various substituents at the N3- and C5-positions were synthesized and their in vitro activity against a panel of clinically relevant MRSA strains was determined. (
  • LFERs can be established only for congeneric series of compounds, i.e., sets of compounds that share the same skeleton and only have variations in the substituents attached to this skeleton. (
  • Bis-benzylidine piperidone compounds, containing alpha,beta-unsaturated carbonyl functionalities, have been extensively documented as being effective in killing apoptosis-resistant cells and to display promising antineoplastic activities in a number of tumor models. (
  • 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. (
  • After discovering a simple, purportedly regioselective reduction of benzylidene acetals using poly-methylhydrosiloxane, we employed this reagent as a part of a broader synthetic scheme. (
  • Benzylidene acetals are used as protecting groups in glycochemistry. (
  • The present invention addresses the problem of providing a compound having a selective inhibitory activity on LAT-1 that can be expressed in a tumor cell at a high level. (
  • The newly synthesized compounds were evaluated for their HIV-1 RT inhibitory activity. (
  • Among the synthesized compounds, compound 24 showed significant HIV-1 RT inhibitory activity with 73% of inhibition with an IC50 value of 1.31 μM. (
  • They found that 1-(2-Bromobenzyloxy)-4-bromo-2-benzylidene rhodanine showed a significant ability to inhibit PRL-3. (
  • 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). (
  • This invention is based on the unexpected discovery that a group of piperazinedione compounds effectively inhibit tyrosine kinase and suppress cancer growth. (
  • 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. (
  • 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. (
  • This invention relates to piperazinedione compounds shown in the specification. (
  • The present invention relates to the antimalarial compounds of formula (l)and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. (
  • The present invention relates to compounds useful as inhibitors of ATR protein kinase. (
  • and solid forms of the compounds of this invention. (
  • The compounds of this invention have formula I-1 or I-A: ##STR00001## wherein the variables are as defined herein. (
  • The method of obtaining the compounds according to the invention is illustrated by the following examples. (
  • 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. (
  • The Amiloxate is a cinnamate ester, Enzacamene is methyl benzylidene camphor and Octyl triazone (Uvinul T150) is a powerful UVB filter that has been used in Europe and elsewhere for some time now. (
  • The title compound, C 10 H 12 N 2 O 2 , was prepared by the reaction of methyl carbazate and 4-methyl-benzaldehyde. (
  • Obtain 1-benzyl-2-[benzylidene)amino] -3-methyl-indole (compound 1). (
  • The determined relative fluorescence quantum yields in solution for both compounds were 0.003 and 0.51, while those in poly(methyl methacrylate) films were around 0.10 and 1.0, respectively. (
  • The stabilizing compounds disclosed are especially applicable and beneficial with respect to sunscreen actives and sunscreen-containing compositions. (
  • Silicone compounds, delivery compositions, compositions, packaged products and displays comprising such silicone compounds, and processes for making and using such benefit agent delivery compositions, compositions, packaged products and displays. (
  • The synthesized compounds were evaluated for their antimicrobial activity. (
  • Curcumin, a yellow polyphenol compound, is known to possess antifungal activity for a range of pathogenic fungi. (
  • The 4-F substituted (E)-1-benzylidene-2-(3-nitrophenyl)hydrazine compound has shown very good antifungal activity against Aspergillus niger. (
  • Compound 10 had most potent antifungal activity against C . albicans and A . niger with MIC = 4.2 × 10 −2 µM/ml. (
  • A series of E-2-benzylidene-1-indanones and E-2-benzlididene-1-benzosuberones were synthesized to investigate their in vitro antifungal activity against 24 strains belonging to important human pathogenic yeasts, such as Cryptococcus neoformans, Candida spp. (
  • 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. (
  • The compound has also been screened for antibacterial and antifungal activity. (
  • The antimicrobial activity results revealed that compound p2 , p3 , p4 and p6 exhibited promising antimicrobial activity that are comparable to standard norfloxacin (antibacterial) and fluconazole (antifungal). (
  • Compounds described are non-imidazole analogs of ciproxifan with a tetralone motif. (
  • 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. (
  • Visual inspection was then performed on the resulting docking solutions of the compound 24 to analyze the binding mode and key protein ligand interactions and was compared with that of the experimentally determined binding mode and interactions of the bound ligand TNK-651 and the standard efavirenz. (
  • KNK437, a benzylidene lactam compound, sensitises prostate cancer cells to the apoptotic effect of hyperthermia. (
  • 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. (
  • Here we generated a new class of sulfonamide-containing compounds that activated HIV-1 in acute and latently infected cells. (
  • Compound 1 exerted an antiangiogenic effect in MCF-7 cells by down-regulating Vascular Endothelial Growth Factor (VEGF) and Hypoxia Inducible Factor-α (HIF-α). (
  • 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. (
  • 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. (
  • class of compounds, the sulphenyl bromides 3, in quantitative yield. (
  • 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. (
  • The synthesized compounds were screened for their in vitro antimicrobial potential against Gram (positive and negative) bacterial and fungal strains by tube dilution technique. (
  • 94 (1982) 134 [I] All the new compounds were characterized by elemental analysis and 'P-NMR spectroscopy (standard: ext. (
  • The structure elucidation of the compound was done by IR and 1HNMR spectroscopy. (
  • this, when heated with silver oxide and water, yields both benzylidene and benzylhydroxide base. (
  • The reaction mixture was cooled for a while and solid separated was filtered and recrystallised from ethanol (99%) yield the title compounds (1-5). (
  • Furthermore UV and IR Spectra of some of the title compounds are also reported. (
  • Title compounds were prepared by the reported method. (
  • Docking study was performed for the highest active compounds by using Glide 5.0. (
  • 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. (
  • The synthesized compound was then evaluated for the antimicrobial activity. (
  • The synthesized compounds were further evaluated for their in vitro antimicrobial activity using turbidimetric method and anticancer activity against oestrogen receptor positive human breast adenocarcinoma cancer cell line (MCF7) by Sulforhodamine B (SRB) assay. (
  • The aromatic substitution reactions are not limited to azobenzene and benzylidene but are even more facile with N,N-dimethylbenzylamine [13,14]. (
  • The target compounds were synthesized from diethyl succinate and benzaldehyde or 4-fluorobenzaldehyde by four-step reactions. (
  • 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. (
  • 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. (
  • 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. (
  • The compound exhibits a combination of catalytic, antibacterial, anti-fouling and adsorptive properties. (
  • The synthesized compounds have been evaluated for their antibacterial and short term anticancer activity. (
  • In the human wild-type (HWT) 5-HT 3A receptor, none of the BA compounds possessed partial agonist activity. (
  • The 4-F substituted compound has shown excellent activity against Enterococcus species and E. (
  • The anti-MRSA activity of compounds 21 (MIC ¼ 3.9 mg/mL, MBC ¼ 7.8 mg/mL) and 22 (MIC ¼ 1.95 mg/mL, MBC ¼ 7.8 mg/mL) was significantly greater than that of the lead compounds, 1e3 and reference antibiotics penicillin G (MIC ¼ 31.25 mg/mL) and ciprofloxacin (MIC ¼ 7.8 mg/mL) and comparable to that of vancomycin (MIC ¼ 0.97 mg/mL). (
  • Compounds 11 and 12, in a concentration-dependent manner, inhibited EGF receptor tyrosine kinase activity. (
  • In assays of adenylyl cyclase activity neither compound 11 nor compound 12 altered Gpp(NH)p- or isoproterenol-stimulated activity. (
  • However, both compounds, in a concentration-dependent manner, attenuated the ability of EGF to stimulate adenylyl cyclase activity without altering specific binding of [125I]EGF to cardiac membranes. (
  • Seventeen compounds had different hypoglycemic activity in mice, among them, 9 compounds had higher hypoglycemic activity and 6 compounds had character of prandial glucose regulator. (
  • Part of the compounds have higher hypoglycemic activity deserve to be further investigated. (
  • Many of the compounds tested were shown to have good activity and many had minimum inhibitory concentrations [MICs] of 6 micro g/ml or lower against most of the strains. (
  • Compounds resulting from microbial activity on plant and animal organic material. (
  • 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. (
  • Structurally related to aurones are benzylidene tetralones, which also possess relatively good A1 and/or A2A AR antagonistic activity and selectivity. (
  • The antimicrobial assay results, show that compounds 4c and 4e highlighted the most interesting profile with the potent activity was obtained against S. enteritidis (1.56-fold) and then M. luteus (1.45-fold) which are significantly higher than the positive control, chloramphenicol. (
  • On the other hand, if you require an accurate estimate of a compound s solubility, a rigorous calculation using the systematic approach and activity coefficients is necessary. (
  • Although they are important compounds that function as cell recognition factors which specifically express these selecting, they are expected to easily lose their activity due to .alpha. (
  • Some of the compounds, such as triptolide, celastrol and demethylzeylasteral from T. wilfordii, have been extensively studied on their mechanisms of action due to their potent activity on various cancer cell lines. (
  • Some of the compounds have shown significant activity. (
  • Schiff base compounds have received much attention because of their potential applications. (
  • 1997). As part of our search for new Schiff base compounds we synthesized the title compound (I), and describe its structure here. (
  • The aim of this concise review is to gather existing literature on anticancer potential of extracts and compounds isolated from Celastraceae species. (
  • Anticancer screening results demonstrated that compound p2 was found to be the most active one against cancer cell line when compared to the rest of the compounds and comparable to the standard drug (5-fluorouracil). (
  • Recently we have developed a panel of small molecular compounds targeting a non-catalytic site of PP1. (
  • These molecular docking results and the way of binding pattern indicated that compounds 7 and 8 bound well within the binding pocket of inhA and showed a higher binding affinity than the known drug isoniazid. (
  • Such promising lead compounds should generate considerable interest among scientists to improve their therapeutic potential with fewer side effects by molecular modification. (
  • The molecular docking study demonstrated that compounds, p2 , p3 , p4 and p6 displayed good docking score within binding pocket of the selected PDB ID (1JIJ, 4WMZ and 3ERT) and showed promising ADME properties. (
  • The minimum inhibitory concentrations of the compounds were also ascertained by agar streak dilution method. (
  • We identify the three distinct structural motifs based on prototypical drugs as the choline motif, the tropane motif, and the benzylidene motif. (
  • These inhibitors represent lead compounds for further development of MtOPRT inhibitors with increased potency, which may be tested as anti-TB agents. (
  • The compounds are potent and/or selective inhibitors of dopamine (DA), serotonin (5-HT), and/or norepinephr. (
  • High-throughput methods for identifying modulators (activators or inhibitors) of HSP or HSF expression in a cell by treating the cell with an agent, such as a compound or composition, exposing the cell to a stress, and measuring responses of the cell to the stress in the presence or absence of the agent are also provided. (
  • The initial lead compound was prepared as a homologue of the 3-benzylidene-1,3-dihydro-2H-indol-2-one class of kinase inhibitor. (
  • Crystallographic analysis of the lead compound bound to CDK2 provided the basis for analogue design. (
  • 7. A microbicidal composition comprising a microbicidally effective amount of a compound or its acid addition salt or metal salt complex as claimed in claim 1 and an inert diluent. (
  • 8. A method for controlling undesired microorganisms in plant protection and in the preservation of materials, which method comprises applying to such undesired microorganisms or to their habitat a microbicidally effective amount of a compound or its acid addition salt or metal salt complex as claimed in claim 1. (
  • The data of elemental analysis, melting points of the synthesized compounds and the parameters of their IR, UV spectra are presented in table 1. (
  • In addition, in general nitro/chloro/furan substituted compounds have been reported to possess various biological activities. (
  • The xanthine core forms the basis of numerous potent and selective A1 and A2A AR antagonists, however, these compounds display low water solubility - limiting their in vivo application. (