Abstract
A series of 4-(2-pyridyl)piperazine-1-benzimidazole analogues based on compound 1 was synthesized and evaluated for TRPV1 antagonist activity in capsaicin-induced (CAP) and pH 5.5-induced (pH) FLIPR assays in a human TRPV1-expressing HEK293 cell line. Potent TRPV1 antagonists were identified through SAR studies. From these studies, several antagonists were found, with IC 50 values ranging from 32 nM to ∼5000 nM. Among these, 11 [IC 50 = 90 nM (CAP) and 104 nM (pH)] was further evaluated and found to be orally available in rats ( F% = 19.7).
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