Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 7651-82-3, is researched, SMILESS is OC1=CC2=C(C=NC=C2)C=C1, Molecular C9H7NOJournal, Article, Journal of Medicinal Chemistry called Novel Vanilloid Receptor-1 Antagonists: 2. Structure-Activity Relationships of 4-Oxopyrimidines Leading to the Selection of a Clinical Candidate, Author is Doherty, Elizabeth M.; Fotsch, Christopher; Bannon, Anthony W.; Bo, Yunxin; Chen, Ning; Dominguez, Celia; Falsey, James; Gavva, Narender R.; Katon, Jodie; Nixey, Thomas; Ognyanov, Vassil I.; Pettus, Liping; Rzasa, Robert M.; Stec, Markian; Surapaneni, Sekhar; Tamir, Rami; Zhu, Jiawang; Treanor, James J. S.; Norman, Mark H., the main research direction is oxopyrimidine TRPV1 antagonist preparation SAR.Quality Control of Isoquinolin-6-ol.
A series of novel 4-oxopyrimidine TRPV1 antagonists was evaluated in assays measuring the blockade of capsaicin or acid-induced influx of calcium into CHO cells expressing TRPV1. The investigation of the structure-activity relationships in the heterocyclic A-region revealed the optimum pharmacophoric elements required for activity in this series and resulted in the identification of subnanomolar TRPV1 antagonists. The most potent of these antagonists were thoroughly profiled in pharmacokinetic assays. Optimization of the heterocyclic A-region led to the design and synthesis of 23 (I), a compound that potently blocked multiple modes of TRPV1 activation. Compound 23 was shown to be effective in a rodent “”on-target”” biochem. challenge model (capsaicin-induced flinch, ED50 = 0.33 mg/kg p.o.) and was antihyperalgesic in a model of inflammatory pain (CFA-induced thermal hyperalgesia, MED = 0.83 mg/kg, p.o.). Based on its in vivo efficacy and pharmacokinetic profile, compound 23 (N-{4-[6-(4-trifluoromethyl-phenyl)-pyrimidin-4-yloxy]-benzothiazol-2-yl}-acetamide; AMG 517) was selected for further evaluation in human clin. trials.
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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method