Substituted biaryl pyrazoles as sodium channel blockers

Voltage-gated sodium channels have been shown to play a critical role in neuropathic pain. A series of low molecular weight biaryl substituted pyrazole carboxamides were identified with good in-vitro potency and in-vivo efficacy. Compound 26, a Nav1.7 blocker has excellent efficacy in the Chung model of neuropathic pain.

A series of low molecular weight biaryl substituted pyrazoles with good in-vitro potency and in-vivo efficacy were identified as Nav1.7 blockers. These state dependent sodium channel blockers were synthesized and evaluated for treatment of neuropathic pain.Figure optionsDownload as PowerPoint slide