Structure–activity relationship (SAR) investigations of substituted imidazole analogs as TRPV1 antagonists

…, R Tamir, NR Gavva, JJS Treanor, MH Norman

文献索引：Gore, Vijay K.; Ma, Vu V.; Tamir, Rami; Gavva, Narender R.; Treanor, James J.S.; Norman, Mark H. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 21 p. 5825 - 5830

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被引用次数: 26

摘要

A novel series of 4, 5-biarylimidazoles as TRPV1 antagonists were designed based on the previously reported 4, 6-disubstituted benzimidazole series. The analogs were evaluated for their ability to block capsaicin-or acid-induced calcium influx in TRPV1-expressing CHO cells. These studies led to the identification of a highly potent and orally bioavailable TRPV1 antagonist, imidazole 33.