Imidazopyridines: a novel class of hNav1.7 channel blockers

  • Bioorg Med Chem Lett. 2008 Mar 1;18(5):1696-701. doi: 10.1016/j.bmcl.2008.01.047.
Clare London  1 ,  Scott B Hoyt ,  William H Parsons ,  Brande S Williams ,  Vivien A Warren ,  Richard Tschirret-Guth ,  McHardy M Smith ,  Birgit T Priest ,  Erin McGowan ,  William J Martin ,  Kathryn A Lyons ,  Xiaohua Li ,  Bindhu V Karanam ,  Nina Jochnowitz ,  Maria L Garcia ,  John P Felix ,  Brian Dean ,  Catherine Abbadie ,  Gregory J Kaczorowski ,  Joseph L Duffy
Affiliations
  • 1. Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. [email protected]
PMID: 18243692 DOI: 10.1016/j.bmcl.2008.01.047
Abstract

A series of imidazopyridines were evaluated as potential Sodium Channel blockers for the treatment of neuropathic Pain. Several members were identified with good hNa(v)1.7 potency and excellent rat pharmacokinetic profiles. Compound 4 had good efficacy (52% and 41% reversal of allodynia at 2 and 4h post-dose, respectively) in the Chung rat spinal nerve ligation (SNL) model of neuropathic Pain when dosed orally at 10mg/kg.