Discovery of 2-(3,5-difluoro-4-methylsulfonaminophenyl)propanamides as potent TRPV1 antagonists.

Changhoon Kim,Jihyae Ann,Sunho Lee,Wei Sun,Peter M Blumberg,Robert Frank-Foltyn,Gregor Bahrenberg,Hannelore Stockhausen,Thomas Christoph,Jeewoo Lee

Bioorganic & Medicinal Chemistry Letters（2018）

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摘要

•A series of A-region analogues of 2-(3-fluoro-4-methylsufonamidophenyl)propanamide were investigated as TRPV1 antagonists.•Compound 6 showed highly potent antagonism toward capsaicin activation.•Compound 6 displayed anti-hypothermic effect and promising analgesic activity in vivo.

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关键词

Vanilloid receptor 1,TRPV1 antagonist,Analgesic

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