Design, synthesis and biological evaluation of N 1 -(isoquinolin-5-yl)-N 2 -phenylpyrrolidine-1,2-dicarboxamide derivatives as potent TRPV1 antagonists.

Mingxiang Gao,Cunbin Nie,Jinyu Li,Beibei Song,Xinru Cheng,Erying Sun,Lin Yan,Hai Qian

Bioorganic Chemistry（2019）

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摘要

Reported herein is the design, synthesis, and pharmacologic evaluation of a class of TRPV1 antagonists constructed on a N1-(isoquinolin-5-yl)-N2-phenylpyrrolidine-1,2-dicarboxamide platform that evolved from a 5-aminoisoquinoline urea lead.

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关键词

Analgesic,Transient receptor potential vanilloid type 1,5-Aminoisoquinoline urea,Hyperthermia

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