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Imidazopyridines: a novel class of hNav1.7 channel blockers |
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| Authors: | London Clare Hoyt Scott B Parsons William H Williams Brande S Warren Vivien A Tschirret-Guth Richard Smith McHardy M Priest Birgit T McGowan Erin Martin William J Lyons Kathryn A Li Xiaohua Karanam Bindhu V Jochnowitz Nina Garcia Maria L Felix John P Dean Brian Abbadie Catherine Kaczorowski Gregory J Duffy Joseph L |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. clare_london@merck.com |
| 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. |
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