Substituted biaryl pyrazoles as sodium channel blockers

S Tyagarajan, PK Chakravarty, B Zhou, B Taylor…

Index: Tyagarajan, Sriram; Chakravarty, Prasun K.; Zhou, Bishan; Taylor, Brett; Fisher, Michael H.; Wyvratt, Mathew J.; Lyons, Kathy; Klatt, Tracy; Li, Xiaohua; Kumar, Sanjeev; Williams, Brande; Felix, John; Priest, Birgit T.; Brochu, Richard M.; Warren, Vivien; Smith, McHardy; Garcia, Maria; Kaczorowski, Gregory J.; Martin, William J.; Abbadie, Catherine; McGowan, Erin; Jochnowitz, Nina; Parsons, William H. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 18 p. 5480 - 5483

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Citation Number: 11

Abstract

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.