Can You Really Do Chemisty Experiments About 5,6-Bis((4-methoxybenzyl)oxy)isobenzofuran-1,3-dione

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N-LINKED HETEROCYCLIC ANTAGONISTS OF P2Y1 RECEPTOR USEFUL IN THE TREATMENT OF THROMBOTIC CONDITIONS

The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.

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Some scientific research about Ethyl benzofuran-2-carboxylate

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Related Products of 3199-61-9, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 3199-61-9, Name is Ethyl benzofuran-2-carboxylate, molecular formula is C11H10O3. In a Article£¬once mentioned of 3199-61-9

Multicomponent cascade reactions for the synthesis of 2,3-dihydrobenzofuran derivatives

A multicomponent cascade reaction for the synthesis of highly substituted 2,3-dihydrobenzofuran derivatives with moderate to good yields was developed. The synthetic utilities of these 2,3-dihydrobenzofurans were also further explored. Ethyl 2-hydroxy-3-oxo-2,3-dihydrobenzofuran-2-carboxylate and ethyl benzofuran-2-carboxylate were easily obtained from 2,3-dihydrobenzofurans.

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Top Picks: new discover of Benzo[b]furan-2-carboxaldehyde

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Synthesis and Evaluation of 2-Pyridinone Derivatives as HIV-1-Specific Reverse Transcriptase Inhibitors. 2. Analogues of 3-Aminopyridin-2(1H)-one

A series of nonnulceoside 3-aminopyridin-2(1H)-one derivatives was synthesized and evaluated for HIV-1 RT inhibitory properties.Several analogs proved to be potent and highly selective antagonists with in vitro IC50 values as low as 19 nM in the enzyme assay using rC*dG as template*primer.Two compounds from this series, 3-<<4,7-dimethylbenzoxazol-2-yl)methyl>amino>-5-ethyl-6-methylpyridin-2(1H)-one (34, L-697,639) and the corresponding 4,7-dichloro analogue (37, L-697,661) inhibited the spread of HIV-1 IIIb infection by 95percent in MT4 cell culture at concentrations of 25-50 nM and were selected for clinical trials as antiviral agents.

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Final Thoughts on Chemistry for 2-(Benzofuran-3-yl)ethanamine

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AZEPINOINDOLE AND PYRIDOINDOLE DERIVATIVES AS PHARMACEUTICAL AGENTS

The present invention is directed to compounds of formula (I) and formula (II): formula (I) and (II), wherein R1-R8, A and n are as described in the description. These compounds are used in pharmaceutical compositions and methods for modulating the activity of orphan nuclear receptors.

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Some scientific research about Benzofuran-2-carboxylic acid

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Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent

Analogs of the previously reported 1,5-benzodiazepine peripheral cholecystokinin (CCK-A) receptor agonist 1 were prepared which explore substitution and/or replacement of the C-3 phenyl urea moiety. Agonist efficacy on the isolated guinea pig gallbladder (GPGB) was retained with a variety of substituted ureas and amide analogs. Three compounds were identified which were orally active in the mouse gallbladder emptying assay (MGBE). The 2-indolamide (52) and N-(carboxymethyl)-2-indolamide (54) derivatives had improved affinity for the human CCK-A receptor but reduced agonist efficacy on the GPGB. Neither indolamide was orally active in a rat feeding assay. In contrast, the (3-carboxyphenyl)urea derivative (29, GW7854) had moderately increased affinity for the human CCK-B receptor but was a potent full agonist on the GPGB and was orally active in both the MGBE and rat feeding assays. GW7854 was a full agonist (EC50 = 60 nM) for calcium mobilization on CHO K1 cells expressing hCCK-A receptors and a potent antagonist of CCK-8 (pA2 = 9.1) on CHO K1 cells expressing hCCK-B receptors. GW7854 is a potent mixed CCK-A agonist/CCK-B antagonist which is orally active in two in vivo models of CCK-A-mediated agonist activity.

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Simple exploration of 496-41-3

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Asymmetric synthesis of a potent azepanone-based inhibitor of the cysteine protease cathepsin K

In this account we detail the asymmetric synthesis of 1, a potent azepanone-based inhibitor of cathepsin K (Ki = 0.16 nM), which has been shown to inhibit the production of biomarkers of bone resorption in monkeys. The key steps in the synthesis sequence were the utility of the Evans aldol reaction coupled with the ring closing olefin metatheses to assemble the azepanone core contained within 1.

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Awesome and Easy Science Experiments about 652-39-1

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Electric Literature of 652-39-1, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 652-39-1, molcular formula is C8H3FO3, introducing its new discovery.

Sarcosine based indandione hGlyT1 inhibitors

A series of sarcosine based indandione hGlyT1 inhibitors has been developed. Optimization of substitution around the indandione and sarcosine moieties has led to highly potent inhibitors at hGlyT1, which show selectivity over a number of other receptors.

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Discovery of 3-Aminobenzofuran-2-carboxamide

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A benzofuran-beta-Alaninamide based “turn-on” fluorescent chemosensor for selective recognition of Fe3+ ions

A benzofuran-beta-Alaninamide based chemosensor, 3-(3-((4-methylbenzyl)amino)propanamido)benzofuran-2-carboxamide (BAA), was designed and synthesized for selective detection of Fe3+ ions. The binding ability of BAA towards Fe3+ in DMSO/H2O solution (9/1, v/v) has been studied by UV-vis absorption and fluorescence spectroscopy. Interestingly, the probe BAA exhibits an excellent “turn-on” fluorescence enhancement at 424 nm with an excitation wavelength of 290 nm. The quantum yield was determined to be 0.248 for BAA and 0.447 for the iron complex. The limit of detection (LOD) was calculated to be 1.3 muM and 0.067 muM by UV-vis absorption and fluorescence methods respectively. These values are much lower than that of US Environmental Protection Agency guidelines for drinking water (5.37 muM). Job’s plot measurement evidenced the 2:1 binding stoichiometry for the complex formed between BAA and Fe3+. Moreover, the binding interaction of BAA towards Fe3+ was confirmed by density functional theory (DFT) studies. Finally, the real sample analysis proved that the probe BAA was more suitable for the detection of Fe3+.

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Some scientific research about 54450-20-3

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Application of 54450-20-3, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.54450-20-3, Name is 5-Bromobenzofuran-3(2H)-one, molecular formula is C8H5BrO2. In a Article£¬once mentioned of 54450-20-3

Organohalogenite-Catalyzed Spiroketalization: Enantioselective Synthesis of Bisbenzannulated Spiroketal Cores

A new core structure-motivated strategy for the intramolecular aromatic spiroketalization process was found and used for the enantioselective synthesis of bisbenzannulated spiroketals, the bioactive core of rubromycins, with high levels of enantioselectivity (up to 98% ee) via an organohalogenite-mediated asymmetric intramolecular aromatic spiroketalization. This is the first organocatalytic method for the construction of optically pure bisbenzannulated spiroketals.

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The important role of 2-Methylbenzofuran

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Sorption of heterocyclic organic compounds to reference soils: Column studies for process identification

In this study, the sorption behavior of a wide variety of N-, S-, and O-heterocyclic compounds (NSOs) to reference soils (Eurosoils 1-5) was characterized by a soil column chromatography (SCC) approach. The major goal was to identify the compound specific and environmental factors influencing sorption processes. The sorption of S- and O-heterocyclic compounds (thiophene, benzothiophene, 5-methylbenzo[b]thiophene, benzofuran, 2-methylbenzofuran, and 2,3-dimethylbenzofuran) was generally controlled by nonspecific interactions with soil organic carbon (OC). With regard to non-ionizable N-heterocyclic compounds, pyrrole, 1-methylpyrrole, and pyrimidine were hardly retarded in any soil. The sorption of indole, 2-hydroxyquinoline, and benzotriazole was dominated by specific interaction (e.g., complexation of surface-bound cations) rather than partition to soil OC. The sorption of ionizable N-heterocyclic compounds (quinoline, isoquinoline, quinaldine, 2-methyl-pyridine, and pyridine) can be described by a conceptual model including partitioning to soil OC, cation exchange, and an additional sorption process (probably surface complexation of the neutral species). Cation exchange was usually the dominant mechanism in the sorption of ionizable compounds if the protonated fraction of the compound exceeded 5%. Otherwise, surface complexation became dominant. Soil pH was the most important factor influencing the sorption of ionizable NSOs. Our study suggests that a fairly precise assessment of sorption in most soils can be expected for N-, S-, and O-heterocyclic compounds if the three sorption mechanisms are taken into account where appropriate. Deviations from this behavior indicated special cases where additional soil specific properties (e.g., accessible surface, CEC, charge density) need to be considered such as for 2-methylpyridine and pyridine sorption to Eurosoil 1.

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