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

Based on a series of diaryl amides the corresponding inverse amides have been found to be potent TRPV1 receptor antagonists. Benzimidazole and indazolone derivatives prepared 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.

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.Figure optionsDownload as PowerPoint slide