The search for novel TRPV1-antagonists: From carboxamides to benzimidazoles and indazolones

Stephen Robert Fletcher,Edward McIver,Stephen Lewis,Frank Burkamp,Clare Leech,Glenn Mason,Susan Boyce,Denise Morrison,Gillian Richards,Kathy Sutton,Anthony Brian Jones

Bioorganic & Medicinal Chemistry Letters（2006）

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摘要

Based on a series of diaryl amides the corresponding inverse amides 2 have been found to be potent TRPV1 receptor antagonists. Benzimidazole (3) and indazolone derivatives (4) retained good potency in vitro and indazolone 4a was identified as a novel TRPV1 receptor antagonist suitable for evaluating orally in animal models of analgesia.

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关键词

TRPV-1 antagonists,Indazolone,Benzimidazole

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