| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374378 | Bioorganic & Medicinal Chemistry Letters | 2006 | 5 Pages |
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.
Graphical abstractBased 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 full-size imageDownload as PowerPoint slide
