Discovery and optimisation of potent and highly subtype selective Nav1.8 inhibitors with reduced cardiovascular liabilities†‡,10.1039/C6MD00281A

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Lactoyl-CoA 全氟丁基戊烷白叶藤碱全氟己基辛烷新白叶藤碱壳寡糖特色专题-生物多肽

Discovery and optimisation of potent and highly subtype selective Nav1.8 inhibitors with reduced cardiovascular liabilities†‡

Sharan K. Bagal,Mark I. Kemp,Peter J. Bungay,Tanya L. Hay,Yoshihisa Murata,C. Elizabeth Payne,Edward B. Stevens,Alan Brown,David C. Blakemore,Matthew S. Corbett,Duncan C. Miller,Kiyoyuki Omoto,Joseph S. Warmus

MedChemComm Pub Date : 07/15/2016 00:00:00 , DOI:10.1039/C6MD00281A

Abstract

Voltage-gated sodium channels, in particular Na_v1.8, can be targeted for the treatment of neuropathic and inflammatory pain. Herein, we describe the discovery and optimisation of a Na_v1.8 inhibiting phenyl imidazole series that delivers chemical equity that possesses high potency and selectivity and is capable of demonstrating good oral pharmacokinetics.