Acetophenonesomega-Chloroacetophenone: A potent eye, throat, and skin irritant. One of its uses is as a riot control agent.Amination: The creation of an amine. It can be produced by the addition of an amino group to an organic compound or reduction of a nitro group.PropiophenonesAmidine-Lyases: These enzymes catalyze the elimination of ammonia from amidines with the formation of a double bond. EC 4.3.2.Amides: Organic compounds containing the -CO-NH2 radical. Amides are derived from acids by replacement of -OH by -NH2 or from ammonia by the replacement of H by an acyl group. (From Grant & Hackh's Chemical Dictionary, 5th ed)Palladium: A chemical element having an atomic weight of 106.4, atomic number of 46, and the symbol Pd. It is a white, ductile metal resembling platinum, and following it in abundance and importance of applications. It is used in dentistry in the form of gold, silver, and copper alloys.PhotochemistryProflavine: Topical antiseptic used mainly in wound dressings.Quantum Theory: The theory that the radiation and absorption of energy take place in definite quantities called quanta (E) which vary in size and are defined by the equation E=hv in which h is Planck's constant and v is the frequency of the radiation.Triplets: Three individuals derived from three FETUSES that were fertilized at or about the same time, developed in the UTERUS simultaneously, and born to the same mother.Rhodocyclaceae: A family of gram-negative bacteria in the order Rhodocyclales, class BETAPROTEOBACTERIA. It includes many genera previously assigned to the family PSEUDOMONADACEAE.Graphite: An allotropic form of carbon that is used in pencils, as a lubricant, and in matches and explosives. It is obtained by mining and its dust can cause lung irritation.Benzene DerivativesOrganic Chemistry Processes: The reactions, changes in structure and composition, the properties of the reactions of carbon compounds, and the associated energy changes.Benzene: Toxic, volatile, flammable liquid hydrocarbon byproduct of coal distillation. It is used as an industrial solvent in paints, varnishes, lacquer thinners, gasoline, etc. Benzene causes central nervous system damage acutely and bone marrow damage chronically and is carcinogenic. It was formerly used as parasiticide.Phloroglucinol: A trinitrobenzene derivative with antispasmodic properties that is used primarily as a laboratory reagent.Dengue Virus: A species of the genus FLAVIVIRUS which causes an acute febrile and sometimes hemorrhagic disease in man. Dengue is mosquito-borne and four serotypes are known.Rutaceae: A plant family in the order Sapindales that grows in warmer regions and has conspicuous flowers.Dengue: An acute febrile disease transmitted by the bite of AEDES mosquitoes infected with DENGUE VIRUS. It is self-limiting and characterized by fever, myalgia, headache, and rash. SEVERE DENGUE is a more virulent form of dengue.Anti-Allergic Agents: Agents that are used to treat allergic reactions. Most of these drugs act by preventing the release of inflammatory mediators or inhibiting the actions of released mediators on their target cells. (From AMA Drug Evaluations Annual, 1994, p475)Mast Cells: Granulated cells that are found in almost all tissues, most abundantly in the skin and the gastrointestinal tract. Like the BASOPHILS, mast cells contain large amounts of HISTAMINE and HEPARIN. Unlike basophils, mast cells normally remain in the tissues and do not circulate in the blood. Mast cells, derived from the bone marrow stem cells, are regulated by the STEM CELL FACTOR.Mallotus Plant: A plant genus of the family EUPHORBIACEAE. Members contain fredelin type TRITERPENES, mallorepine (a cyano-pyridone), and hydrolyzable TANNINS.Hydrogenation: Addition of hydrogen to a compound, especially to an unsaturated fat or fatty acid. (From Stedman, 26th ed)Iridium: A metallic element with the atomic symbol Ir, atomic number 77, and atomic weight 192.22.Stereoisomerism: The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)Ruthenium: A hard, brittle, grayish-white rare earth metal with an atomic symbol Ru, atomic number 44, and atomic weight 101.07. It is used as a catalyst and hardener for PLATINUM and PALLADIUM.KetonesCatalysis: The facilitation of a chemical reaction by material (catalyst) that is not consumed by the reaction.Alcohols: Alkyl compounds containing a hydroxyl group. They are classified according to relation of the carbon atom: primary alcohols, R-CH2OH; secondary alcohols, R2-CHOH; tertiary alcohols, R3-COH. (From Grant & Hackh's Chemical Dictionary, 5th ed)China: A country spanning from central Asia to the Pacific Ocean.Carboxyl and Carbamoyl Transferases: A group of enzymes that catalyze the transfer of carboxyl- or carbamoyl- groups. EC 2.1.3.Erythroxylaceae: A plant family of the order Linales, subclass Rosidae, class Magnoliopsida best known for the coca plant.Refractometry: Measurement of the index of refraction (the ratio of the velocity of light or other radiation in the first of two media to its velocity in the second as it passes from one into the other).Viscosity: The resistance that a gaseous or liquid system offers to flow when it is subjected to shear stress. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)Chemistry, Pharmaceutical: Chemistry dealing with the composition and preparation of agents having PHARMACOLOGIC ACTIONS or diagnostic use.Blood Viscosity: The internal resistance of the BLOOD to shear forces. The in vitro measure of whole blood viscosity is of limited clinical utility because it bears little relationship to the actual viscosity within the circulation, but an increase in the viscosity of circulating blood can contribute to morbidity in patients suffering from disorders such as SICKLE CELL ANEMIA and POLYCYTHEMIA.IndiaFraud: Exploitation through misrepresentation of the facts or concealment of the purposes of the exploiter.Counterfeit Drugs: Drugs manufactured and sold with the intent to misrepresent its origin, authenticity, chemical composition, and or efficacy. Counterfeit drugs may contain inappropriate quantities of ingredients not listed on the label or package. In order to further deceive the consumer, the packaging, container, or labeling, may be inaccurate, incorrect, or fake.Skin Irritancy Tests: Tests or bioassays that measure the skin sensitization potential of various chemicals.Culture Media: Any liquid or solid preparation made specifically for the growth, storage, or transport of microorganisms or other types of cells. The variety of media that exist allow for the culturing of specific microorganisms and cell types, such as differential media, selective media, test media, and defined media. Solid media consist of liquid media that have been solidified with an agent such as AGAR or GELATIN.Irritants: Drugs that act locally on cutaneous or mucosal surfaces to produce inflammation; those that cause redness due to hyperemia are rubefacients; those that raise blisters are vesicants and those that penetrate sebaceous glands and cause abscesses are pustulants; tear gases and mustard gases are also irritants.Glass: Hard, amorphous, brittle, inorganic, usually transparent, polymerous silicate of basic oxides, usually potassium or sodium. It is used in the form of hard sheets, vessels, tubing, fibers, ceramics, beads, etc.Pulmonary Artery: The short wide vessel arising from the conus arteriosus of the right ventricle and conveying unaerated blood to the lungs.Glyburide: An antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.Phenylephrine: An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.Mannich Bases: Ketonic amines prepared from the condensation of a ketone with formaldehyde and ammonia or a primary or secondary amine. A Mannich base can act as the equivalent of an alpha,beta unsaturated ketone in synthesis or can be reduced to form physiologically active amino alcohols.Adhesives: Substances that cause the adherence of two surfaces. They include glues (properly collagen-derived adhesives), mucilages, sticky pastes, gums, resins, or latex.Administration, Cutaneous: The application of suitable drug dosage forms to the skin for either local or systemic effects.Pressure: A type of stress exerted uniformly in all directions. Its measure is the force exerted per unit area. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)Transducers, Pressure: Transducers that are activated by pressure changes, e.g., blood pressure.Hydrostatic Pressure: The pressure due to the weight of fluid.Silicones: 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)Leeches: Annelids of the class Hirudinea. Some species, the bloodsuckers, may become temporarily parasitic upon animals, including man. Medicinal leeches (HIRUDO MEDICINALIS) have been used therapeutically for drawing blood since ancient times.

Arachidonic acid, but not its metabolites, is essential for FcgammaR-stimulated intracellular killing of Staphylococcus aureus by human monocytes. (1/833)

Since arachidonic acid (AA) production by phospholipase A2 (PLA2) is essential for the Fcgamma receptor (FcgammaR)-mediated respiratory burst and phagocytosis of opsonized erythrocytes by monocytes and macrophages, we focused in this study on the role of AA and its metabolites in the FcgammaR-stimulated intracellular killing of Staphylococcus aureus by human monocytes. The results revealed that the PLA2 inhibitors, but not inhibitors of cyclo-oxygenase and lipoxygenase, markedly suppressed the FcgammaR-mediated killing process. The production of O-2 by monocytes upon FcgammaR cross-linking was inhibited by 4-bromophenacyl bromide in a dose-dependent fashion, indicating that inhibition of PLA2 activity impairs the oxygen-dependent bactericidal mechanisms of monocytes, which could be partially restored by addition of exogenous AA and docosahexaenoic acid, but not myristic acid. These polyunsaturated fatty acids, but not myristic acid, stimulated the intracellular killing of S. aureus by monocytes, although not as effectively as FcgammaR cross-linking. Furthermore, FcgammaR cross-linking stimulated the release of AA from monocytes. Studies with selective inhibitors revealed that the FcgammaR-mediated activation of PLA2 is dependent on Ca2+ and tyrosine kinase activity. Together these results indicate a key role for PLA2/AA, but not its major metabolites, in mediating the FcgammaR-stimulated intracellular killing of S. aureus by monocytes.  (+info)

Protein kinase Cdelta mediates neurogenic but not mitogenic activation of mitogen-activated protein kinase in neuronal cells. (2/833)

In several neuronal cell systems, fibroblast-derived growth factor (FGF) and nerve growth factor (NGF) act as neurogenic agents, whereas epidermal growth factor (EGF) acts as a mitogen. The mechanisms responsible for these different cellular fates are unclear. We report here that although FGF, NGF, and EGF all activate mitogen-activated protein (MAP) kinase (extracellular signal-related kinase [ERK]) in rat hippocampal (H19-7) and pheochromocytoma (PC12) cells, the activation of ERK by the neurogenic agents FGF and NGF is dependent upon protein kinase Cdelta (PKCdelta), whereas ERK activation in response to the mitogenic EGF is independent of PKCdelta. Antisense PKCdelta oligonucleotides or the PKCdelta-specific inhibitor rottlerin inhibited FGF- and NGF-induced, but not EGF-induced, ERK activation. In contrast, EGF-induced ERK activation was inhibited by the phosphatidylinositol-3-kinase inhibitor wortmannin, which had no effect upon FGF-induced ERK activation. Rottlerin also inhibited the activation of MAP kinase kinase (MEK) in response to activated Raf, but had no effect upon c-Raf activity or ERK activation by activated MEK. These results indicate that PKCdelta functions either downstream from or in parallel with c-Raf, but upstream of MEK. Inhibition of PKCdelta also blocked neurite outgrowth induced by FGF and NGF in PC12 cells and by activated Raf in H19-7 cells, indicating a role for PKCdelta in the neurogenic effects of FGF, NGF, and Raf. Interestingly, the PKCdelta requirement is apparently cell type specific, since FGF-induced ERK activation was independent of PKCdelta in NIH 3T3 murine fibroblasts, in which FGF is a mitogen. These data demonstrate that PKCdelta contributes to growth factor specificity and response in neuronal cells and may also promote cell-type-specific differences in growth factor signaling.  (+info)

Translocation of protein kinase Cepsilon and protein kinase Cdelta to membrane is required for ultraviolet B-induced activation of mitogen-activated protein kinases and apoptosis. (3/833)

UV-induced signal transduction may be involved in tumor promotion and induction of apoptosis. The role of protein kinase C (PKC) in UVB-induced signal transduction is not well understood. This study showed that UVB markedly induced translocation of membrane-associated PKCepsilon and PKCdelta, but not PKCalpha, from cytosol to membrane. Dominant negative mutant (DNM) PKCepsilon or PKCdelta inhibited UVB-induced translocation of PKCepsilon and PKCdelta, respectively. UVB-induced activation of extracellular signal-regulated protein kinases (Erks) and c-Jun NH2-terminal kinases (JNKs) was strongly inhibited by DNM PKCepsilon and PKCdelta, whereas the DNM of PKCalpha was less effective on the UVB-induced phosphorylation of Erks and JNKs. Among the PKC inhibitors used only rottlerin, a selective inhibitor of PKCdelta, markedly inhibited the UVB-induced activation of Erks and JNKs, but not p38 kinases. Safingol, a selective inhibitor for PKCalpha, did not show any inhibitory effect on UVB-induced mitogen-activated protein kinase activation. GF109203X is a stronger inhibitor of classical PKC than novel PKC. Lower concentrations of GF109203X (<10 microM) had no effect on UVB-induced activation of Erks or JNKs. However, at higher concentrations (over 20 microM), GF109203X inhibited UVB-induced activation of JNKs, Erks, and even p38 kinases. Meanwhile, rottlerin and GF109203X markedly inhibited UVB-induced apoptosis of JB6 cells, whereas safingol had little inhibitory effect. DNM-Erk2 cells and PD98059, a selective inhibitor for mitogen-activated protein kinase/extracellular signal-regulated kinase 1 that directly activates Erks, inhibited UVB-induced apoptosis. DNM-JNK1 cells also blocked UVB-induced apoptosis, whereas SB202190, a specific inhibitor for p38 kinases, did not produce the inhibitory effect. These data demonstrate that PKCdelta and PKCepsilon, but not PKCalpha, mediate UVB-induced signal transduction and apoptosis in JB6 cells through activation of Erks and JNKs.  (+info)

Odor response properties of rat olfactory receptor neurons. (4/833)

Molecular biology studies of olfaction have identified a multigene family of molecular receptors that are likely to be involved in odor transduction mechanisms. However, because previous functional data on peripheral coding were mainly collected from inferior vertebrates, it has been difficult to document the degree of specificity of odor interaction mechanisms. As a matter of fact, studies of the functional expression of olfactory receptors have not demonstrated the low or high specificity of olfactory receptors. In this study, the selectivity of olfactory receptor neurons was investigated in the rat at the cellular level under physiological conditions by unitary extracellular recordings. Individual olfactory receptor neurons were broadly responsive to qualitatively distinct odor compounds. We conclude that peripheral coding is based on activated arrays of olfactory receptor cells with overlapping tuning profiles.  (+info)

Protein kinase C delta is essential for etoposide-induced apoptosis in salivary gland acinar cells. (5/833)

We have previously shown that parotid C5 salivary acinar cells undergo apoptosis in response to etoposide treatment as indicated by alterations in cell morphology, caspase-3 activation, DNA fragmentation, sustained activation of c-Jun N-terminal kinase, and inactivation of extracellular regulated kinases 1 and 2. Here we report that apoptosis results in the caspase-dependent cleavage of protein kinase C-delta (PKCdelta) to a 40-kDa fragment, the appearance of which correlates with a 9-fold increase in PKCdelta activity. To understand the function of activated PKCdelta in apoptosis, we have used the PKCdelta-specific inhibitor, rottlerin. Pretreatment of parotid C5 cells with rottlerin prior to the addition of etoposide blocks the appearance of the apoptotic morphology, the sustained activation of c-Jun N-terminal kinase, and inactivation of extracellular regulated kinases 1 and 2. Inhibition of PKCdelta also partially inhibits caspase-3 activation and DNA fragmentation. Immunoblot analysis shows that the PKCdelta cleavage product does not accumulate in parotid C5 cells treated with rottlerin and etoposide together, suggesting that the catalytic activity of PKCdelta may be required for cleavage. PKCalpha and PKCbeta1 activities also increase during etoposide-induced apoptosis. Inhibition of these two isoforms with Go6976 slightly suppresses the apoptotic morphology, caspase-3 activation, and DNA fragmentation, but has no effect on the sustained activation of c-Jun N-terminal kinase or inactivation of extracellular regulated kinase 1 and 2. These data demonstrate that activation of PKCdelta is an integral and essential part of the apoptotic program in parotid C5 cells and that specific activated isoforms of PKC may have distinct functions in cell death.  (+info)

Dual efficacy of lamivudine treatment in human immunodeficiency virus/hepatitis B virus-coinfected persons in a randomized, controlled study (CAESAR). The CAESAR Coordinating Committee. (6/833)

The efficacy and safety of lamivudine in persons coinfected with human immunodeficiency virus (HIV) type 1 and hepatitis B virus (HBV) were examined in the CAESAR study, a randomized placebo-controlled trial assessing the addition of lamivudine (150 mg 2x/day) or lamivudine (150 mg 2x/day) plus loviride (100 mg 3x/day) to zidovudine-containing background antiretroviral treatment. Baseline hepatitis B surface antigen (HBsAg) results were available for 1790 study subjects, of whom 122 (6.8%) tested positive. Retrospective analyses for serial HBV DNA, HBsAg, and hepatitis B e antigen (HBeAg) were performed on stored sera from 118 HBsAg-positive subjects. HBV DNA and HBeAg were present in 83% and 63%, respectively. At weeks 12 and 52, median log10 HBV DNA change was -2.0 and -2.7, respectively, in the lamivudine arms, compared with no reduction among placebo recipients (P<.001). A trend to lower alanine transferase level, and delayed progression of HIV-1 disease (relative hazard, 0.26; 95% confidence interval, 0.08-0.80) were also seen in the lamivudine arms, compared with the placebo group.  (+info)

Apocynin improves diaphragmatic function after endotoxin administration. (7/833)

Free radicals are known to play an important role in modulating the development of respiratory muscle dysfunction during sepsis. Moreover, neutrophil numbers increase in the diaphragm after endotoxin administration. Whether or not superoxide derived from infiltrating white blood cells contributes to muscle dysfunction during sepsis is, however, unknown. The purpose of the present study was to examine the effect of apocynin, an inhibitor of the superoxide-generating neutrophil NADPH complex, on endotoxin-induced diaphragmatic dysfunction. We studied groups of rats given saline, endotoxin, apocynin, or both endotoxin and apocynin. Animals were killed 18 h after injection, a portion of the diaphragm was used to assess force generation, and the remaining diaphragm was used for determination of 4-hydroxynonenal (a marker of lipid peroxidation) and nitrotyrosine levels (a marker of free radical-mediated protein modification). We found that endotoxin reduced diaphragm force generation and that apocynin partially prevented this decrease [e.g., force in response to 20 Hz was 23 +/- 1 (SE), 12 +/- 2, 23 +/- 1, and 19 +/- 1 N/cm(2), respectively, for saline, endotoxin, apocynin, and endotoxin/apocynin groups; P < 0.001]. Apocynin also prevented endotoxin-mediated increases in diaphragm 4-hydroxynonenal and nitrotyrosine levels (P < 0.01). These data suggest that neutrophil-derived free radicals contribute to diaphragmatic dysfunction during sepsis.  (+info)

Theoretical elucidation of activity differences of five phenolic antioxidants. (8/833)

AIM: To verify the effectiveness of structure-activity relationship (SAR) and theoretical calculation methods for antioxidants. METHODS: Preliminary elucidation on the differences of activities of 5 antioxidants was performed by SAR. Then semiempirical quantum chemistry method AM1 was employed to calculate the delta HOF value, the difference between the heat of formation of antioxidant and its free radical, which was used as a theoretical parameter to elucidate the differences of activities of the antioxidants thoroughly. RESULTS: delta HOF values of antioxidants were obtained as follows: ferulic acid, 150.58 kJ.mol-1; anion of ferulic acid, 122.64 kJ.mol-1; modified ferulic acid, 137.70 kJ.mol-1; anion of modified ferulic acid, 118.99 kJ.mol-1; salvianic acid, 134.17 kJ.mol-1; rutin, 137.83 kJ.mol-1, L-EGCG, 124.39 kJ.mol-1; paeonol, 176.79 kJ.mol-1. The differences of the antioxidant activities were elucidated, and how to further enhance the antioxidant activity was investigated as well. CONCLUSION: The SAR and calculation methods are rather effective to elucidate the differences of antioxidant activities, and present some new clues for structural modification of antioxidants to increase their activities.  (+info)

4-AMINOACETOPHENONE OXIME 38063-81-9 NMR spectrum, 4-AMINOACETOPHENONE OXIME H-NMR spectral analysis, 4-AMINOACETOPHENONE OXIME C-NMR spectral analysis ect.
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Detail záznamu - Effect of chronic apocynin treatment on nitric oxide and reactive oxygen species production in borderline and spontaneous hypertension - Detail záznamu - Knihovna Akademie věd České republiky
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Compared to the currently available therapeutic drugs for peripheral vascular diseases, agents that are selective for relaxing pulmonary circulation are scarce. The present study was undertaken, using isometric tension change measurement and whole-cell patch-clamp electrophysiology methods, to evaluate the vascular relaxation effect and the underlying mechanisms involved of two naturally found alkaloids: paeonol (2-hydroxy-4-methoxy-acetophenone), acetovanillone (4-hydroxy-3-methoxy-acetophenone) and the non-substituted analogue acetophenone on pulmonary artery of Sprague-Dawley rats. Cumulative administration (3 μM-1 mM) of acetophenone analogues resulted in a concentration-dependent relaxation of phenylephrine (1 μM) pre-contracted pulmonary artery. A relative order of inhibitory potency, estimated by comparing the concentration at which a 50% relaxation of phenylephrine-induced contraction observed was: acetovanillone , paeonol , acetophenone. Endothelial denudation and inhibition of nitric ...
Hydroxyacetophenone (HAP, CAS 99-93-4) Market by Product (2-Hydroxyacetophenone, 4-Hydroxyacetophenone), by Application (Pharmaceuticals, Chemical Intermediates, Cosmetics) and by Region, Trend, Forecast, Competitive Analysis, and Growth Opportunity 2019-2024 - Radiant Insights
Cheung S-Y, Werner M, Esposito L, Troisi F, Cantone V, Liening S, König S, Gerstmeier J, Koeberle A, Bilancia R, Rizza R, Rossi A, Roviezzo F, Temml V, Schuster D, Stuppner H, Schubert-Zsilavecz M, Werz O, Hanke T, Pace S (2018) Discovery of a benzenesulfonamide-based dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase that favorably modulates lipid mediator biosynthesis in inflammation. Eur J Med Chem 156:815-830. ...
E.R.T., Tiekink, (2015) A crystallographic and computational study of 1-(arylamino)-1,2,3-triazole-4-carbohydrazides. CrystEngComm, 17. pp. 2255-2266. E.R.T., Tiekink, (2015) Bipodal benzoylthiocarbamic acid esters: Crystal and molecular structures of R = Et (a polymorph), and of a binuclear Cu(I) complex, R = iPr. Zeitschrift Fur Kristallographie, 230. pp. 397-405. E.R.T., Tiekink, (2015) Conformational preferences for isomeric N,N-bis(pyridin-n-ylmethyl)ethanedithio-diamides, n = 2, 3 and 4: A combined crystallographic and DFT study. Zeitschrift Fur Kristallographie-Crystalline Materials, 230. pp. 531-541. E.R.T., Tiekink, (2015) Conformational study of some 4-substituted 2-(phenylselanyl)-2-(ethylsulfonyl)- acetophenones. Journal of Molecular Structure, 1084. pp. 190-199. E.R.T., Tiekink, (2015) Crystal structure of catena-poly[(u2-chlorido)-bis(N-ethyl,N-hydroxyethylcarbamo-dithioato-u2S,S)bismuth(III) monohydrate], C10H22BiClN2O3S4. Zeitschrift Fur Kristallographie-New Crystal ...
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Lamani, M. and Prabhu, K. R. (2012), NIS-Catalyzed Reactions: Amidation of Acetophenones and Oxidative Amination of Propiophenones. Chem. Eur. J., 18: 14638-14642. doi: 10.1002/chem.201202703 ...
Diabetic nephropathy is the main cause for initiation of renal replacement therapy and early symptoms in patients include increased glomerular filtration rate (GFR), decreased oxygen tension and albuminuria, followed by a progressive decline in GFR and loss of kidney function. Experimental models of diabetes display increased GFR, decreased tissue oxygenation and nitric oxide bioavailability. These findings are likely to be intertwined in a mechanistic pathway to kidney damage and this thesis investigated their roles in the development of diabetic nephropathy. In vivo, diabetes-induced oxidative stress stimulates renal tubular Na+ transport and in vitro, proximal tubular cells from diabetic rats display increased transport-dependent oxygen consumption, demonstrating mechanisms contributing to decreased kidney oxygenation. In control animals, endogenous adenosine reduces vascular resistance of the efferent arteriole via adenosine A2-receptors resulting in reduced filtration fraction. However, in ...
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2,4-dihydroxyacetophenone (10.64 g, 0.07 mol) and potassium hydroxide (10.58 g, 0.189 mol) were dissolved in dry acetone (100 ml) in a three-neck flask. Then ethyl bromoacetate (28.06 g, 0.168 mol) was dropwise added at room temperature and vigorously stirred for 3 h. The progress of the reaction was monitored by TCL (Si gel, developing solvent V (acetone) /V (petroleum ether) = 1:2). After suction filtration and distillation to remove the solvent, a white solid was obtained, 19.76 g, yield 87.1%. This solid was dissolved in acetone (30 ml) and 20% aq. NaOH (50 ml) was added. The reaction mixture was stirred at 323 K for 1.5 h. After acidifying the misxture with dilute hydrochloric acid to pH=3, followed by suction filtrationand washing the residue with water, the target product was prepared. After recrystallization from ethanol, crystalline colorless needles were obtained.. ...
Human being monoclonal antibodies (HMAbs) with neutralizing capabilities constitute potential immune-based remedies or prophylaxis against hepatitis C disease (HCV). in BSF 208075 support of three HMAbs (HC-1AM, HC84.24, and AR4A) neutralized all 16 HCVcc recombinants. Furthermore, the IC50-ideals for confirmed HMAb assorted using the HCVcc stress significantly, which supports the usage of a varied disease panel. In assistance analyses, HMAbs HC84.24, AR3A, and, hC84 especially.26, demonstrated synergistic results towards a lot of the HCVccs when combined individually with AR4A. Through a neutralization evaluation of 10 relevant HMAbs against 16 JFH1-centered Core-NS2 recombinants from genotypes 1a medically, 1b, 2a, 2b, 2c, and 3a, we identified at least 3 HMAbs with wide and powerful neutralization potential. The neutralization synergism acquired when pooling the strongest HMAbs could possess significant implications for developing novel ways of deal with and control HCV. transfection and ...
Examples of effect: Lead to damage to heath, cause irritation to eyes, skin or respiratory organs. Are fatal in larger quantities. Safety: As previously stated, in the event of skin irritation or contact with eyes, rinse with water or a suitable medium. ...
Examples of effect: Lead to damage to heath, cause irritation to eyes, skin or respiratory organs. Are fatal in larger quantities. Safety: As previously stated, in the event of skin irritation or contact with eyes, rinse with water or a suitable medium. ...
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Oxidative stress is a major mediator of cellular injury following ischaemic stroke and reactive oxygen species, like superoxide, have multiple deleterious effects on the components of the neurovascular unit. It is well established that NADPH oxidase is the principal source of superoxide in acute ischaemic stroke and is therefore a target for potential neuroprotective strategies (Moskowitz et al, 2010). Consequently, the second aim of this thesis was to evaluate the potential neuroprotective effect of NADPH oxidase inhibition with low and high dose apocynin following permanent or transient ischaemia. Rats were administered apocynin at a dose of 5mg/kg or 30mg/kg or vehicle, at 5 minutes post-MCAO. Apocynin treatment had no significant effect on infarct volume or functional outcome at 24 hours following permanent MCAO in WKY rats. However, both low and high dose apocynin treatment significantly reduced infarct volume at 72 hours post-MCAO by 60% following 1 hour of ischaemia in Sprague-Dawley ...
Pro-apoptotic protein kinase C delta is associated with intranuclear inclusions in a transgenic model of Huntingtons disease.: In order to investigate any effe
Cyclooxygenase-2 (COX-2) and its metabolite prostaglandin E2 (PGE2) can potentially affect most of the events in cancer development, including promotion of proliferation, resistance to apoptosis, angiogenesis, immune suppression and invasion. However, worldwide attention has predominantly centered on the cardiovascular toxicity of selective COX-2 inhibitors. Paeonol is a major active extract from the root bark of Paeonia suffruticosa Andrews with anti‑inflammatory, anti-oxidant, anti-allergic, anti-oxidation and antitumor effects. In the present study, we investigated the underlying mechanisms of paeonol in inducing apoptosis and aimed to ascertain whether its antitumor effect is associated with a reduction in COX-2 expression and a decrease in the levels of PGE2 in colorectal cancer cells. We observed that paeonol inhibited cell proliferation and induced apoptosis in a dose- and time-dependent manner in colorectal cancer cells, which was associated with a reduction in COX-2 expression and ...
The molecular mechanisms and signaling pathways that get -cell compensation and failure are not fully resolved islet. FoxO1 in Pdx1-harmful -cells (14, 17). FoxO1 activity is certainly modulated by post-translational adjustments and protein-protein connections that influence its intracellular trafficking and function (18). In the -cell, development or insulin aspect PI3T/Akt-induced FoxO1 phosphorylation qualified prospects to its translocation from the nucleus to cytoplasm, alleviating its inhibition of focus on gene transcription (14). The incretin human hormones GIP and glucagon-like peptide 1 (GLP-1) also activate this series (19, 20). Another is certainly the stability between oxidative stress-induced FoxO1 acetylation and deacetylation (21). Hence, FoxO1 orchestrates -cell transcriptional regulatory paths for adaptive replies to many human hormones, development elements, and metabolic challenges. Whereas very much is certainly known about FoxO1 activity in -cells, very much much less is ...
This research is proposed in response to NIH Notice Number PA-07-320 (Development of assays for high-throughput drug screening). We have found that anti-oxidant...
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Inhibition of 4E-BP phosphorylation and function by perhexiline, niclosamide, amiodarone and rottlerin.MCF-7 cells stably expressing EGFP-LC3 were incubated wit
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Flavones are widely distributed in nature and have been found to associated with a variety of biological activities as anticarcinogen, antiinflammatory and antifungals etc. The commonly used synthetic methods of flavone derivatives are as follows; the Kostanecki reaction, the Baker-venkataraman method, synthesis from chalcone, synthesis via an intramolecular Wittig strategy and lithiation reaction. In the present study, flavone derivatives containing methoxy or methyl groups were prepared by the following three steps; The first step was the synthesis of ortho-acetylphenylbenzoate derivatives from 2-hydroxyacetophenone derivatives and benzoyl chloride derivatives with DMAP as base in dichloroethane at 80℃. The second step was the intramolecular claisen condensation to form 1-(2-hydroxypheny1)-1,3-propanedione derivatives from ortho-acetylphenylbenzoate derivatives using potassium tert-butoxide in THF at 67℃. The third step was dehydrative cyclization to get the desired flavone derivatives ...
Melford Laboratories Ltd. is a leading supplier and manufacturer of research chemicals and biochemicals. Melford Laboratories Ltd. has over 300 chemicals in stock including plant tissue culture media, Biological buffers, and agarose. Melford Laboratories Ltd. are enzyme substrate suppliers that have the lowest prices in the industry on popular compounds IPTG �8/GM, X-Gal �30/GM, X-GlcA �54/100MG. Melford Laboratories Ltd. has a range of over 55 antibiotics which include hard to find compounds Zeocin and Cycloheximide. Research Melford Laboratories Ltd. has 17 years of experience manufacturing 4-Mu Substrates. Melford Laboratories Ltd. is best known for Fluorochemicals. Melford Laboratories Ltd. has methodology for the manufacture of numerous compound types, including Phenylhydrazines, Benzylamines, Benzaldhydes, Acetophenones, Sulphonyl chlorides, Bezonitriles, Benzyl alcohols, and Benzyl bromides.
Melford Laboratories Ltd. is a leading supplier and manufacturer of research chemicals and biochemicals. Melford Laboratories Ltd. has over 300 chemicals in stock including plant tissue culture media, Biological buffers, and agarose. Melford Laboratories Ltd. are enzyme substrate suppliers that have the lowest prices in the industry on popular compounds IPTG �8/GM, X-Gal �30/GM, X-GlcA �54/100MG. Melford Laboratories Ltd. has a range of over 55 antibiotics which include hard to find compounds Zeocin and Cycloheximide. Research Melford Laboratories Ltd. has 17 years of experience manufacturing 4-Mu Substrates. Melford Laboratories Ltd. is best known for Fluorochemicals. Melford Laboratories Ltd. has methodology for the manufacture of numerous compound types, including Phenylhydrazines, Benzylamines, Benzaldhydes, Acetophenones, Sulphonyl chlorides, Bezonitriles, Benzyl alcohols, and Benzyl bromides.
1. A scheme of synthesis was developped for cholecystokinin (CCK 26-33, using solid-phase methodology and successfully applied to the synthesis of its C- and N-terminal fragments. 2. Using CCK 30-33 as model, it was found that deprotection of the ?-phenacyl ester, with a 1 M solution of sodium thiophenoxide in DMF, leads to the formation of an aminosuccylnyl peptide, prior to ammonolysis. 3. Selenophenol reagent successfully removes the ?-phenacyl ester on protected CCK 32-33 and on protected CCK 30-33 polymer prior to ammonolytic cleavage of peptides from the resin. 4. Treatment of Boc-Asp(?-OPac)-Tyr(0-2,4-Dnp)-Met-Gly-Trp(Nin-For)-Met-Asp(?-OPac)-Phe-polymer with a 1 M solution of selenophenol in DMF, leads to irreversible rearrangement of the 0-2,4-dinitrophenyl ether. 5. Undesirable side-reactions can be avoided by sequential deprotections and cleavage. The 0-2,4-dinitrophenyl ether is removed by thiolysis following by selenolysis of the ?-phenacyl esters. Cleavage of the peptide from the ...
In atherosclerosis, local generation of reactive oxygen species amplifies the inflammatory response and contributes to plaque vulnerability. We used molecular imaging to test whether inhibition of NADPH oxidase with apocynin would reduce endothelial inflammatory activation and endothelial-platelet interactions, thereby interrupting progression to high-risk plaque phenotype. METHODS AND RESULTS: Mice deficient for both the low-density lipoprotein receptor and Apobec-1 were studied at 30 weeks of age and again after 10 weeks with or without apocynin treatment (10 or 50 mg/kg per day orally). In vivo molecular imaging of vascular cell adhesion molecule-1 (VCAM 1) P-selectin, and platelet glycoprotein-1balpha (GPIbalpha) in the thoracic aorta was performed with targeted contrast-enhanced ultrasound molecular imaging. Arterial elastic modulus and pulse wave transit time were assessed using ultrahigh frequency ultrasound and invasive hemodynamic measurements. Plaque size and composition were assessed ...
TY - JOUR. T1 - NADPH oxidase inhibitors. T2 - A decade of discovery from Nox2ds to HTS. AU - Cifuentes-Pagano, Eugenia. AU - Csanyi, Gabor. AU - Pagano, Patrick J.. PY - 2012/7/1. Y1 - 2012/7/1. N2 - NADPH oxidases (Nox) are established as major sources of reactive oxygen species (ROS). Over the past two decades, Nox-derived ROS have emerged as pivotal in the development of myriad diseases involving oxidative stress. In contrast, Nox are also involved in signaling mechanisms necessary for normal cell function. The study of these enzymes in physiological and pathophysiological conditions is made considerably more complex by the discovery of 7 isoforms: Nox1 through 5 as well as Duox1 and 2, each with its own specific cytosolic components, regulatory control mechanisms, subcellular localization and/or tissue distribution. A clear understanding of the role individual isoforms play in a given system is hindered by the lack of isoform-specific inhibitors. In animal models, knockdown or knockout ...
Possible factors regulating the opening of and the rate of H+ flux through a recently described, Cd(2+)-sensitive, phorbol ester- and arachidonic acid (AA)-activatable H(+)-conducting pathway in the plasma membrane of neutrophil granulocytes were investigated. (1) The phospholipase A2 blocker p-bromophenacyl bromide (BPB) inhibited the phorbol 12-myristate 13-acetate (PMA)-induced activation of this channel in a concentration-dependent manner (IC50, 4 microM). (2) Neither BPB nor the protein kinase C (PKC) inhibitor staurosporine influenced the AA-elicited stimulation of this route. (3) Intracellular acidification (cytoplasmic pH below 6.9) itself is capable of activating an electrogenic, Cd(2+)-sensitive H+ efflux indicating that protons can open up this route in the absence of any other stimulator. (4) PMA significantly decreases the intracellular H+ concentration ([H+]i) threshold for the opening of the channel, thus providing a conductive state at resting pH values, and elevates the rate of ...
Densities, viscosities, refractive indices and ultrasonic velocities of the binary mixtures of Acetophenone with Propyl acetate were measured over the entire mole fractions at (303.15, 313.15 and 323.15) K. From these experimental results, excess molar volumes VE, viscosity deviation ∆η, refractive index deviation ∆nD, deviations in isentropic compressibility ∆Ks and excess intermolecular free length ∆Lf are calculated. The viscosity values were fitted to the models of Krishnan- Laddha and McAllister. The thermo physical properties under study were fit to the Jouyban - Acree model. The excess values were correlated using Redlich-Kister polynomial equation to obtain their coefficients and standard deviations. It was found that in all cases, the data obtained fitted with the values correlated by the corresponding models very well. The results are interpreted in terms of molecular interactions occurring in the solution.
After the bromine has been added the ether and dissolved hydrogen bromide are removed at once (Note 4) under reduced pressure with a slight current of air. The phenacyl bromide remains as a solid mass of brownish yellow crystals (Note 5); the color is removed by shaking with a mixture of 10 cc. of water and 10 cc. of petroleum ether. The crystals are filtered with suction and washed several times with fresh portions of the solvent mixture, if necessary, until a white product is obtained (Note 6). The crude phenacyl bromide weighs 74-80 g. (88-96 per cent of the theoretical amount) and melts at 45-48°. This material is sufficiently pure for many purposes. If higher purity is desired the crude product may be recrystallized from 25-30 cc. of methanol, yielding 54-55 g. (64-66 per cent of the theoretical amount) of white crystals melting at 49-51° (Note 7) ...
NADPH oxidases are a family of enzymes that generate reactive oxygen species (ROS). The NOX1 (NADPH oxidase 1) and NOX2 oxidases are the major sources of ROS in the artery wall in conditions such as hypertension, hypercholesterolaemia, diabetes and ageing, and so they are important contributors to the oxidative stress, endothelial dysfunction and vascular inflammation that underlies arterial remodelling and atherogenesis. In this Review, we advance the concept that compared to the use of conventional antioxidants, inhibiting NOX1 and NOX2 oxidases is a superior approach for combating oxidative stress. We briefly describe some common and emerging putative NADPH oxidase inhibitors. In addition, we highlight the crucial role of the NADPH oxidase regulatory subunit, p47phox, in the activity of vascular NOX1 and NOX2 oxidases, and suggest how a better understanding of its specific molecular interactions may enable the development of novel isoform-selective drugs to prevent or treat cardiovascular ...
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Other reasons of circulatory decompensation, such as pulmonary embolism, cardiac tamponade or pulmonary diseases, were excluded. Studies on the biosynthesis of precursors of viagra alternatives glycinebetaine in seedlings of wheat (Triticum vulgare vill.). The proposed echocardiographic multidimensional MR grading system is feasable and shows good correlation with invasive grading.. Nematicidal activity of acetophenones and chalcones against Meloidogyne incognita and structure-activity viagra connect considerations. We conducted a systematic review and statistical analysis of historical data concerning vaccination against smallpox with different strains of vaccinia virus.. Seven subjects from each group who had slightly different SSCP patterns were selected for sequencing, but we found no TLR4 polymorphisms on Exon3. Clusters of cultures sildenafil side effects can then be observed by doing a cluster analysis on the (co)variance matrices of sets of related items. No classifiers could ...
Even though time-dependent density-functional theory (TDDFT) works generally well for describing excited states energies and properties in the Franck-Condon region, it can dramatically fail in predicting photochemistry, notably when electronic state crossings occur. Here, we assess the ability of TDDFT to describe the photochemistry of an important class of triplet sensitizers, namely, aromatic ketones. We take acetophenone as a test molecule, for which accurate ab initio results exist in the literature. Triplet acetophenone is generated thanks to an exotic three-state crossing involving one singlet and two triplets states (i.e., a simultaneous intersystem crossing and triplet conical intersection), thus being a stringent test for approximate TDDFT. We show that most exchange-correlation functionals can only give a semi-qualitative picture of the overall photochemistry, in which the three-state crossing is rather represented as a triplet conical intersection separated from the intersystem ...
1. Paeonol, the primary active component of a traditional Chinese medicine Moutan Cortex, has a wide range of pharmacological activities. In the present study, the metabolism of paeonol by cytochrome P450s (CYPs) was investigated in human liver microsomes ...
In this paper, the optimal composition of a paeonol temperature-sensitive in situ gel composed of poloxamer 407 (P407) was determined, and a preliminary study of its effect on allergic rhinitis was performed. The optimal composition of the paeonol temperature-sensitive in situ gel included 2% paeonol inclusion, 22% P407, 2% poloxamer 188 (P188) and 2% PEG6000, as assessed by thermodynamic and rheological studies. The toad palate model was employed to study the toxicity of the paeonol temperature-sensitive in situ gel on the nasal mucosa. The result of this experiment showed low toxicity to cilia, which allows the gel to be used for nasal administration. The Franz diffusion cell method was used to study the in vitro release of paeonol and suggested that the in vitro release was in line with the Higuchi equation. This result suggests that the paeonol could be absorbed into the body through mucous membranes and had some characteristics of a sustained effect. Finally, the guinea pig model of ovalbumin
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To investigate whether apocynin, a NADPH oxidase inhibitor, produced cardioproteictive effects in Ang II-induced hypertensive mice, and to elucidate the underlying mechanisms. C57BL/6 mice were subcutaneously infused Ang II for 4 weeks to mimic
Apocynin, an inhibitor of NADPH-oxidase, is known to partially reverse the inflammation-mediated cartilage proteoglycan synthesis in chondrocytes. More recently, it was reported that apocynin prevents cyclooxygenase (COX)-2 expression in monocytes. The present study aimed to investigate whether these in vitro features of apocynin could be confirmed in vivo. In a mouse model of zymosan-induced acute arthritis apocynin was administered orally (0, 3.2, 16 and 80 microg/ml in the drinking water) and the effects on cartilage proteoglycan synthesis were monitored. In a mouse model of zymosan-induced inflammation of the ears apocynin was administered orally (14 mg/kg/day by gavage) and the effects on ear swelling and ex vivo produced prostaglandin E2 (PGE2) by lipopolysaccharide (LPS)-stimulated blood cells were measured. In this study, ibuprofen was used as a positive control (50 mg/kg/day by gavage) and animals received vehicle as a negative control. Apocynin dose-dependently reversed the inhibition ...
Antineoplastics, PI3K Delta InhibitorsThis drug class inhibits one or more of the phosphoinositide 3-kinase enzymes, which are part of the PI3K/AKT/mTOR pathway, an important signalling pathway for ma... more
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Outbreaks of spruce budworm (SBW, Choristoneura fumiferana Clem.) cause major recurrent damage in boreal conifers such as white spruce (Picea glauca [Moench] Voss) and large losses of forest biomass in North America. Although defensive phenolic compounds have recently been linked to chemical resistance against SBW, their genetic basis remains poorly understood in forest trees, especially in conifers. Here, we used diverse association genetics approaches to discover genes and their variants that may control the accumulation of acetophenones, and dissect the genetic architecture of these defence compounds against SBW in white spruce mature trees. Out of 4747 single nucleotide polymorphisms (SNPs) from 2312 genes genotyped in a population of 211 unrelated individuals, genetic association analyses identified 35 SNPs in 33 different genes that were significantly associated with the defence traits by using single-locus, multi-locus and multi-trait approaches. The multi-locus approach was particularly
We have demonstrated that BK- or CCh-induced reduction in MVO2 was attenuated in nNOS−/− compared with WT mice. Acute inhibition of nNOS with SMTC or 7-NI did not affect BK-induced reduction in MVO2 in WT mice. The attenuated control of MVO2 in nNOS−/− mice was restored by preincubation with Tiron, Tempol, ascorbic acid, oxypurinol, or SB203580. There was an increase in lucigenin-detectable O2− production in cardiac muscle from nNOS−/− compared with WT mice, which was inhibited by oxypurinol or SB203580. There was no difference in eNOS, iNOS, and XO/XDH protein levels between WT and nNOS−/− mice. Very interestingly, there was an increase in phosphorylated p38 kinase protein level in nNOS−/− compared with WT mice. Therefore, we concluded that a defect of nNOS attenuated control of MVO2 by NO derived from another source most likely eNOS, which is associated with an increase in O2− through the activation of XO, and XO was posttranslationally activated through a mechanism ...
The present studies demonstrate that the organic nitrate PETN but not ISMN improves vascular function and reduces oxidative stress via inhibition of vascular superoxide production in mitochondria and by inhibition of the vascular NADPH oxidase in an experimental model of AT-II-induced hypertension. In almost all of the animal models where endothelial dysfunction is encountered, such as atherosclerosis,23 chronic congestive heart failure,24 AT-II-induced hypertension,4 and diabetes mellitus,25 we established that increased production of ROS via activation of the vascular NADPH oxidase and xanthine oxidase contributed considerably to this phenomenon. Interestingly, in all of the models, eNOS expression was upregulated rather than downregulated, suggesting that eNOS might be dysfunctional, as uncoupled under these circumstances.4,23-25. Previously, it was conceptualized that treatment with an exogenous source of NO (eg, GTN) could compensate for the diminished endothelial NO availability in ...
Oxidative stress is involved in the pathogenesis of a number of diseases including hypertension and renal failure. There is enhanced expression of nicotinamide adenine dinucleotide (NADPH oxidase) and therefore production of hydrogen peroxide (H2O2) during renal disease progression. This study investigated the effect of apocynin, an NADPH oxidase inhibitor and catalase, an H2O2 scavenger on Cyclosporine A (CsA) nephrotoxicity in Wistar-Kyoto rats. Rats received CsA (25mg/kg/day via gavage) and were assigned to vehicle, apocynin (2.5mmol/L p.o.), catalase (10,000U/kg/day i.p.) or apocynin plus catalase for 14 days. Renal functional and hemodynamic parameters were measured every week, and kidneys were harvested at the end of the study for histological and NADPH oxidase 4 (NOX4) assessment. Oxidative stress markers and blood urea nitrogen (BUN) were measured. CsA rats had higher plasma malondialdehyde (by 340%) and BUN (by 125%), but lower superoxide dismutase and total antioxidant capacity (by ...
In this study, synthesis of acetophenone as a widely used industrial compound was investigated by liquid phase oxidation of ethylbenzene with TBHP as an oxidant in acetonitrile over Pd/g-C3N4-rGO as a recyclable catalyst. The hybrid composite of graphitic carbon nitride (g-C3N4) and reduced graphene oxide (r
Lipopolysaccharide (LPS)-mediated endothelial activation plays a part in lung swelling and alveolar remodeling observed in premature babies with bronchopulmonary dysplasia (BPD). at 11,000 0.05 was considered significant for tests. For 2-OH-E+ measurements, log10 changed data were likened between LPS-treated and control cells using an unpaired and and = 0.006 (control vs. LPS-treated), = 3. = 0.03 (control vs. 4 h LPS- treated); ##= 0.002 (control vs. 24 h LPS-treated), = 4. = 0.001 (control vs. 12 h LPS); $$= 0.001 (control vs. 24 h LPS), = 4. Aftereffect of NADPH-oxidase activity manipulation on LPS-mediated endothelial activation. To determine FJX1 whether LPS-induced endothelial activation can be Nox reliant, we utilized complementary 956104-40-8 manufacture techniques (chemical substance inhibitors and siRNA). Apocynin, a substance that may quench superoxide or become a Nox inhibitor, attenuated LPS-mediated ICAM-1 manifestation by 50% (Fig. 2, and and and = 0.001 (control vs. LPS); ##= ...
virA and virG are the Ti-plasmid functions required for chemotaxis of Agrobacterium tumefaciens towards acetosyringone (pages 413-417). C. H. Shaw, A. M. Ashby, A. Brown, C. Royal, G. J. Loake and C. M. Shaw. Version of Record online: 27 OCT 2006 , DOI: 10.1111/j.1365-2958.1988.tb00046.x. ...
Multiple lines of evidence support the idea that autophagy plays an essential role in the development of drug resistance, self-renewal, differentiation, and tumorigenic potentials of cancer stem cells (CSCs). Rottlerin (ROT) is widely used as a protein kinase C-delta (PKC-δ) inhibitor. Recent studies revealed that ROT induces apoptosis through engagement of mitochondria. However, it is not known whether ROT-induced apoptosis is associated with other mechanisms such as autophagy. Here we found that ROT induced autophagy followed by induction of apoptosis via inhibition of PI3K/Akt/mTOR pathway and activation of caspase cascade in human pancreatic CSCs. ROT induced a dose- and time-dependent inhibition of cell survival and induction of cytoplasmic vacuolations. The conversion of microtubule-associated protein LC3-I to LC3-II, and increased accumulations of Atg7 and Beclin-1 were also observed in CSCs treated with ROT. Prolonged exposure of CSCs to ROT eventually caused apoptosis which was ...
Beginning at 20 minutes all hearts received full flow reperfusion at 85 mm Hg for 15 minutes. Fluorescence (F/F0) and rate pressure product (RPP) were calculated as a fraction of baseline and analyzed with ANOVA. At reperfusion, in the Low Flow group fluorescein F/F0 was decreased (0.577 ± 0.039 vs. 1.081 ± 0.060, p,0.001) and resorufin F/F 0 was increased (1.375 ± 0.012 vs. 1.115 ± 0.014, p,0.001) compared to the No Flow group. RPP, at the end of reperfusion, was improved in Low Flow hearts compared to No Flow (0.75 ± 0.07 vs. 0.87± 0.02, p=0.1). In the presence of apocynin, resorufin F/F0 at reperfusion was decreased in both groups (p,0.001) and RPP was significantly improved in the low flow group (p,0.01). Low coronary flow prior to full reperfusion mediates a compartment specific ROS response which is associated with improved recovery of LV function. NADPH oxidase inhibition attenuates the low flow induced amplification of vascular ROS, further improving recovery of LV function. This ...
It is well known that COPD is a preventable and treatable disease, characterized by not fully reversible airflow limitation. In individuals with COPD, there is a marked exacerbation of the inflammatory response, which increases with the progression of the disease. The molecular mechanism of exacerbations remains unknown; however, prolonged oxidative stress have been reported as potentially responsible for the exacerbation. Apocynin is an agent that inhibits activation of an enzyme responsible for ROS generation and thus - probably, alleviate inflammatory process.. Therefore, we investigated the effect of nebulized apocynin in fourteen COPD patients in placebo-controlled, cross-over design study. Exhaled breath condensate was collected in three timepoints (30, 60 and 120 min.) after apocynin/placebo application and H2O2 NO2- and NO3- concentrations have been evaluated. Moreover, safety parameters have been controlled throughout the study.. Apocynin reduced hydrogen peroxide concentration in ...
In early test tube and mouse studies, investigators at Johns Hopkins Medicine and the Johns Hopkins Kimmel Cancer Center have found that nonmuscle myosin IIC (MYH14), a protein activated in response to mechanical stress, helps promote metastatic behavior in pancreatic cancer cells, and that the compound 4-hydroxyacetophenone (4-HAP), known to stiffen myosin IIC-containing cells, can send it into overdrive, overwhelming the ability of cells to invade nearby tissue.
ORLANDO, Fla., Dec. 07, 2015-- TG Therapeutics, Inc., today announced the presentation of updated clinical results from its ongoing Phase I single agent study of TGR-1202, the Company s next generation PI3K delta inhibitor, as well as its Phase II combination study of TG-1101, the Company s novel, glycoengineered monoclonal antibody plus ibrutinib, the oral BTK...
tHGA is a geranyl acetophenone originally found in the young leaves of Melicope ptelefolia. It is also a phloroglucinol compound that contains phloroglucinols as its common monomer unit [31]. Previous studies have reported that tHGA, at 5 and 20 μM, exerts anti-allergic properties by preserving the morphology of MCs and attenuating the release of pro-inflammatory mediators in both cellular and animal model of IgE-mediated MC activation whereby inhibition of β-hexosaminidase and TNF-α were reported [18]. However, our results in the present study revealed that this phloroglucinol compound was unable to attenuate the release of both β-hexosamidase and TNF-α inflammatory by the DENV3-induced RBL-2H3 cells. It is possible that tHGA may not target the signaling molecules involved in the mechanism of action (MOA) of direct DENV infection in MCs. As tHGA has been previously reported to target the linker for activation of T cell, which is located along the classical signaling pathway of MC ...
Abstract : P-Hydroxyacetophenone (PHAP) is an aromatic ketone derivative that is mainly used in the manufacturing of various pharmaceuticals, flavours, fragrances, etc. In the present study, the impact of Mr. Trivedis biofield energy treatment was analysed on various properties of PHAP viz. crystallite size, surface area, melting temperature, thermal decomposition, and spectral properties. The PHAP sample was divided into two parts; one was kept as control sample while another part was named as treated sample. The treated sample was given the biofield energy treatment and various parameters were analysed as compared to the control sample by X-ray diffraction (XRD), surface area analyser, thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), ultravioletvisible (UV-VIS), and Fourier transform infrared (FT-IR) spectroscopy. The XRD studies showed the decrease in crystallite size of the treated sample (61.25 nm) as compared to the control (84.18 nm); however the intensity of ...
In this study we confirmed that NO may induce HO-1 expression and provided a novel mechanism by which NO modulates NADPH oxidase-dependent superoxide production. This mechanism of NADPH oxidase suppression is supported by the following findings: (1) an NO donor consistently induced HO-1 expression; (2) the NO donor suppressed superoxide-generating capacity of NADPH oxidase, an effect distinct from a direct neutralizing action of NO; (3) the inhibitory effect of NO was abolished by cotreatment with HO-1 inhibitors; and (4) bilirubin, the metabolic product of HO-1, mimicked the effect of NO. The current results do not exclude the possibility that NO acts via other mechanisms to suppress NADPH oxidase activation, which can be achieved with the NO donor at concentrations ,30 μmol/L, as reported previously in neutrophils24 and more recently by our group in HMECs.9 In the present study, however, a direct inhibition of NADPH oxidase function is unlikely to be the predominant mechanism, because the ...
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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 ...
Authors: NESLİHAN DEMİRBAŞ, AHMET DEMİRBAŞ, HAKAN BEKTAŞ, ŞENGÜL ALPAY KARAOĞLU, DENİZ ŞAHİN Abstract: The synthesis of 4-amino-2-[(5-mercapto-1,3,4-oxadiazol-2- yl)methyl]-5-(4-methylphenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one (2) and 4-amino-2-[(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)methyl]- 5-(4-methylphenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one (5) was performed starting from 2-[4-amino-3-(4-methylphenyl)-5-oxo-4,5- dihydro-1H-1,2,4-triazol-1-yl]acetohydrazide (1). The treatment of 2 and 5 with 4-fluorobenzaldehyde (for 8) or salicylaldehyde (for 6) afforded the corresponding Schiff bases (6 and 8). The condensation of 5 with phenacyl bromide produced 4-amino-5-(4-methylphenyl)-2- [(6-phenyl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazin-3-yl)methyl]- 2,4-dihydro-3H-1,2,4-triazol-3-one (7). The alkylation of 2 and 8 was carried out by using methyl iodide in basic media. Compounds 3 and 10a,b were prepared by aminoalkylation of 2 and 8 with 4-fluorophenyl piperazine, morpholine, or ...
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Learn about the structure and functions of NADPH (Nicotinamide Adenine Dinucleotide Phosphate) in human body as well is process of its formation.
TG Therapeutics PI3K delta inhibitor, umbralisib, put up encouraging phase 2b data in marginal zone lymphoma, shrinking tumors in more than half of the patients followed long enough to be evaluated. Of these patients, nearly one-fifth were in complete remission, that is, their cancer was undetectable after treatment.
TG Therapeutics PI3K delta inhibitor, umbralisib, put up encouraging phase 2b data in marginal zone lymphoma, shrinking tumors in more than half of the patients followed long enough to be evaluated. Of these patients, nearly one-fifth were in complete remission, that is, their cancer was undetectable after treatment.
Acetophenone Butyrophenone Propiophenone Klan P.; Janosek J.; Krz Z. (2000). "Photochemistry of valerophenone in solid ...
... is a substituted acetophenone. It is a useful building block in organic chemistry. Apart from that, it has ...
The α-bromination of acetophenone with bromine. Liesegang rings Autocatalytic surface growth of metal nanoparticles in solution ...
In one example, mice were conditioned to fear a strong scent, acetophenone, by accompanying the smell with an electric shock. ... Consequently, the mice learned to fear the scent of acetophenone alone. It was discovered that this fear could be passed down ... Despite the offspring never experiencing the electric shock themselves the mice still display a fear of the acetophenone scent ...
... acetophenone, and related substances". American Chemical Journal. 42 (6): 477-498. Hocking, M. B.; Bhandari, K.; Shell, B.; ...
Coordination of another acetophenone molecule regenerates complex 2. Kakiuchi, Fumitoshi; Kochi, Takuya (2008-10-01). " ... acetophenone coordinates to the complex via its carbonyl oxygen and agostically via its ortho C-H bond (2). As in the Ru0 ...
Acetophenone (C6H5C(O)CH3) is an asymmetrical ketone. In the area of stereochemistry, asymmetrical ketones are known for being ...
The drug is the ketal formed between algestone and acetophenone. Algestone acetophenide is said to be both more potent and ...
70, p. 35 (1992). Article Reaction of acetophenone with methylamine in Organic Syntheses, Coll. Vol. 6, p. 818 (1988); Vol. 54 ...
1887). 'Cases Illustrating the Sedative Effects of Aceto-phenone (hypnone)'. Journal of Mental Science. 32: 519-25. (1887). ' ...
... acetophenones". Arkivoc. 2005 (6): 356-365. doi:10.3998/ark.5550190.0006.631. Zhang, Y; Kensler, TW; Cho, CG; Posner, GH; ...
"Phenyl-tetrazolyl acetophenones: discovery of positive allosteric potentiatiors for the metabotropic glutamate 2 receptor". ...
The methyl group of acetophenone was brominated with bromine to give α-bromoacetophenone, which was then reacted with N- ... A synthesis using "classical" methodology was reported by Durden and co-workers, starting from acetophenone. ...
Compounds isolated from the plant include flavonoids, sesquiterpenoids, monoterpenoids, acetylenes, p-acetophenones, ...
The result indicated that the products contain styrene, acetophenone and brominated substances. The report was published by ...
... the latter of which quickly breaks down to acetophenone. Acetophenone is then reduced to an alcohol and conjugated by ... Chlorfenvinphos is produced by reaction of triethylphosphite (P(OEt)3) with 2,2,2,4-tetrachloro acetophenone (C8H4Cl4O). In the ...
Products of decomposition of cumene hydroperoxide are methylstyrene, acetophenone, and cumyl alcohol. Its formula is C6H5C(CH3) ...
This method lead to the reduction of substituted acetophenones in up to 83%ee (Figure 5). The appeal of this method is that it ...
Alternatively, it can also be prepared by oxidation of acetophenone with selenium dioxide. Kenji Takahashi (1968). "The ...
Babu S, Raghavamenon AC, Fronczek FR, Uppu RM (2009). "4-Hydr-oxy-3-meth-oxy-5-nitro-aceto-phenone (5-nitro-apocynin)". Acta ...
estimate 0.9 kg of AlCl3 is wasted per kilogram of dimethyl acetophenone produced. Product separation can also be difficult. ...
In the second reaction sequence, [Carbonyl-14C]-2-hydroxy-acetophenone was used first. Compound XII was formed from ... condensation of [carbonyl-14C-]-2-hydroxy-acetophenone with dimethyl oxylate and ring closure. Hydrogenolytical debenzylation ...
The structure contains acetophenone and a polyyne portions, conjugated together as an ynone. Capillin is found in the essential ...
The result indicated that the products contain styrene, acetophenone, and brominated substances, which can negatively affect ...
It is prepared using acetophenone, formaldehyde, and an amine hydrochloride in a Mannich reaction. It can be polymerized to ...
... in the process with a small amount of by-product acetophenone. Acetophenone is recovered or hydrogenated to 1-phenylethanol ... Acetophenone is the organic compound with the formula C6H5C(O)CH3 (also represented by the pseudoelement symbols PhAc or BzMe ... Acetophenone is an ingredient in fragrances that resemble almond, cherry, honeysuckle, jasmine, and strawberry. It is used in ... In a 1994 report released by five top cigarette companies in the U.S., acetophenone was listed as one of the 599 additives to ...
Acetophenone carboxylase (EC 6.4.1.8) is an enzyme with systematic name acetophenone:carbon-dioxide ligase (ADP-forming). This ... Acetophenone carboxylase at the US National Library of Medicine Medical Subject Headings (MeSH) Molecular and Cellular Biology ... Jobst, B.; Schuhle, K.; Linne, U.; Heider, J. (2010). "ATP-dependent carboxylation of acetophenone by a novel type of ... enzyme catalyses the following chemical reaction 2 ATP + acetophenone + HCO3− + H2O + H+ ⇌ {\displaystyle \rightleftharpoons } ...
Acetophenone Butyrophenone Propiophenone Klan P.; Janosek J.; Krz Z. (2000). "Photochemistry of valerophenone in solid ...
Phenacyl chloride is a substituted acetophenone. It is a useful building block in organic chemistry. Apart from that, it has ...
The α-bromination of acetophenone with bromine. Liesegang rings Autocatalytic surface growth of metal nanoparticles in solution ...
Coordination of another acetophenone molecule regenerates complex 2. Kakiuchi, Fumitoshi; Kochi, Takuya (2008-10-01). " ... acetophenone coordinates to the complex via its carbonyl oxygen and agostically via its ortho C-H bond (2). As in the Ru0 ...
Acetophenone (C6H5C(O)CH3) is an asymmetrical ketone. In the area of stereochemistry, asymmetrical ketones are known for being ...
The drug is the ketal formed between algestone and acetophenone. Algestone acetophenide is said to be both more potent and ...
70, p. 35 (1992). Article Reaction of acetophenone with methylamine in Organic Syntheses, Coll. Vol. 6, p. 818 (1988); Vol. 54 ...
1887). Cases Illustrating the Sedative Effects of Aceto-phenone (hypnone). Journal of Mental Science. 32: 519-25. (1887). ...
... acetophenones". Arkivoc. 2005 (6): 356-365. doi:10.3998/ark.5550190.0006.631. Zhang, Y; Kensler, TW; Cho, CG; Posner, GH; ...
"Phenyl-tetrazolyl acetophenones: discovery of positive allosteric potentiatiors for the metabotropic glutamate 2 receptor". ...
... acetophenone, and related substances". American Chemical Journal. 42 (6): 477-498. Hocking, M. B.; Bhandari, K.; Shell, B.; ...
Consequently, the mice learned to fear the scent of acetophenone alone. It was discovered that this fear could be passed down ... In one example, mice were conditioned to fear a strong scent, acetophenone, by accompanying the smell with an electric shock. ... Despite the offspring never experiencing the electric shock themselves the mice still display a fear of the acetophenone scent ...
Compounds isolated from the plant include flavonoids, sesquiterpenoids, monoterpenoids, acetylenes, p-acetophenones, ...
The result indicated that the products contain styrene, acetophenone and brominated substances. The report was published by ...
... the latter of which quickly breaks down to acetophenone. Acetophenone is then reduced to an alcohol and conjugated by ... Chlorfenvinphos is produced by reaction of triethylphosphite (P(OEt)3) with 2,2,2,4-tetrachloro acetophenone (C8H4Cl4O). In the ...
Products of decomposition of cumene hydroperoxide are methylstyrene, acetophenone, and cumyl alcohol. Its formula is C6H5C(CH3) ...
This method lead to the reduction of substituted acetophenones in up to 83%ee (Figure 5). The appeal of this method is that it ...
Alternatively, it can also be prepared by oxidation of acetophenone with selenium dioxide. Kenji Takahashi (1968). "The ...
Babu S, Raghavamenon AC, Fronczek FR, Uppu RM (2009). "4-Hydr-oxy-3-meth-oxy-5-nitro-aceto-phenone (5-nitro-apocynin)". Acta ...
estimate 0.9 kg of AlCl3 is wasted per kilogram of dimethyl acetophenone produced. Product separation can also be difficult. ...
In the second reaction sequence, [Carbonyl-14C]-2-hydroxy-acetophenone was used first. Compound XII was formed from ... condensation of [carbonyl-14C-]-2-hydroxy-acetophenone with dimethyl oxylate and ring closure. Hydrogenolytical debenzylation ...
The structure contains acetophenone and a polyyne portions, conjugated together as an ynone. Capillin is found in the essential ...
It is prepared using acetophenone, formaldehyde, and an amine hydrochloride in a Mannich reaction. It can be polymerized to ...
  • We are one of the leading manufacturer of Acetophenone, 4-methoxy-3-nitro benzoic acid, 4-chloro-3-nitor- benzooic acid, 2-cloro and 5 nitro benjoic acid , organic intermediates and bulk drugs like benzophenones, acetophenones, ester, acids & amides, quaternary ammonium salts inorganic salt. (exportersindia.net)
  • This invention relates to novel substituted acetophenones and derivatives thereof, processes for the preparation thereof, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments. (patentsencyclopedia.com)
  • In view of the unexpected behavior of α-(benzenesulfonyl)-acetophenone toward hydrolysis and because of the possible physiological importance of its derivatives it was deemed of interest to make a further study of the hydrolysis of this compound. (unt.edu)
  • The Swamping Catalyst Effect in Bromination of Acetophenone" which, as the term he coined implies, describes the use of larger amounts of catalyst to "supercharge" chemical reactions which were subsequently driven to produce greater amounts of product. (wikipedia.org)
  • For example, in a study involving acetophenones this oxygen was preferentially inserted in-between the carbonyl and the aromatic ring to give acetyl aromatic esters, not methyl benzoates. (wikipedia.org)
  • In addition, the proposed catalyst also retained its activity and selectivity for acetophenone after 5 runs. (rsc.org)
  • Although no mechanistic rationale was offered at the time, Brunner was the first to report that hydrosilylation of acetophenone in the presence of a chiral phosphine-copper catalyst afforded enantioenriched product (up to 40% ee). (wikipedia.org)
  • 1 1H NMR S pectra : 1) 5-chloro -2-hydroxy acetophenone thiosemicarbazone ( L) (Fig. Favorsky Irkutsk. (corso-massaggiobari.it)
  • Engaged in supplying and export of Acetophenone, 4-methoxy acetophenone acrylic acid butylated hydroxy anisole-bha calcium gluconate calcium lactate di ethyl malonate etc. (exportersindia.net)
  • The present study was undertaken, using isometric tension change measurement and whole-cell patch-clamp electrophysiology methods, to evaluate the vascular relaxation effect and the underlying mechanisms involved of two naturally found alkaloids: paeonol (2-hydroxy-4-methoxy-acetophenone), acetovanillone (4-hydroxy-3-methoxy-acetophenone) and the non-substituted analogue acetophenone on pulmonary artery of Sprague-Dawley rats. (edu.au)
  • In 1894, Niementowski reported that 2-phenyl-4-hydroxyquinoline was formed when anthranilic acid and acetophenone were heated to 120-130 °C. He later found that at higher heat, 200 °C, anthranilic acid and heptaldehyde formed minimal yields of 4-hydroxy-3-pentaquinoline. (wikipedia.org)
  • Separation of the active ingredients from diarylheptanoids and phloracetophenone glucoside compounds were carried out and some active compounds, such as 1,7-diphenyl-5-hydroxy-(1E)-1-heptene and 4,6-dihydroxy-2-o-(b-D-glucopyranosyl) acetophenone, were found to have a stimulative effect on bile secretion in rats. (wikipedia.org)
  • Here, we used diverse association genetics approaches to discover genes and their variants that may control the accumulation of acetophenones, and dissect the genetic architecture of these defence compounds against SBW in white spruce mature trees. (biomedcentral.com)
  • No changes or were observed in the placebo group p and acetophenone appeared to have entangled no effect essay on the pharmacokinetics of porfimer sodium. (utidur.com)
  • Densities, viscosities, refractive indices and ultrasonic velocities of the binary mixtures of Acetophenone with Propyl acetate were measured over the entire mole fractions at (303.15, 313.15 and 323.15) K. From these experimental results, excess molar volumes V E , viscosity deviation ∆η, refractive index deviation ∆n D , deviations in isentropic compressibility ∆K s and excess intermolecular free length ∆L f are calculated. (sapub.org)
  • Acetophenone and propyl acetate mixture was used in the manufacture of cosmetics amd fruit flavouring agents. (sapub.org)
  • In continuation of this research, we have reported density ( ρ ), viscosity ( η ), refractive index ( n D ) and sound speed ( u ) of pure acetophenone and propyl acetate for the binary system constituted by these two chemicals at temperatures of 303.15, 313.15 and 323.15 K. The viscosity values have been fitted to McAllister and Krishnan and Laddha model. (sapub.org)
  • Female ants of this species can also reproduce through thelytokous parthenogenesis, but, unlike most ant species during this process, the individual will rupture the membrane of the gaster, causing a burst of secretions containing their offspring in addition to acetophenones and other chemicals. (wikipedia.org)
  • Illustrative of its nucleophilicity, anisole reacts with acetic anhydride to give 4-methoxyacetophenone: CH3OC6H5 + (CH3CO)2O → CH3OC6H4C(O)CH3 + CH3CO2H Unlike most acetophenones, but reflecting the influence of the methoxy group, methoxyacetophenone undergoes a second acetylation. (wikipedia.org)
  • Hippuric acid occurs as an indirect metabolite and its quantity in urine may be used to confirm acetophenone exposure, although other substances, like toluene, also induce hippuric acid in urine. (wikipedia.org)
  • Acetophenone is an important industrial chemical widely used as an ingredient of flavour and fragrance in soaps, detergents, cosmetics and perfumes. (sapub.org)
  • Acetosyringone is a phenolic natural product, and is a chemical compound related to acetophenone and 2,6-dimethoxyphenol. (wikipedia.org)
  • Density, Viscosity, and Speed of Sound of (1-Octanol + 2-Methoxyethanol),(1-Octanol + N,N-Dimethylacetamide), and (1-Octanol + Acetophenone) at Temperatures of (298.15, 308.15, and 318.15) K". Journal of Chemical & Engineering Data. (wikipedia.org)