Bioorganic & Medicinal Chemistry Letters 2007-11-15

Benzazepinone Nav1.7 blockers: potential treatments for neuropathic pain.

Scott B Hoyt, Clare London, Hyun Ok, Edward Gonzalez, Joseph L Duffy, Catherine Abbadie, Brian Dean, John P Felix, Maria L Garcia, Nina Jochnowitz, Bindhu V Karanam, Xiaohua Li, Kathryn A Lyons, Erin McGowan, D Euan Macintyre, William J Martin, Birgit T Priest, McHardy M Smith, Richard Tschirret-Guth, Vivien A Warren, Brande S Williams, Gregory J Kaczorowski, William H Parsons

Index: Bioorg. Med. Chem. Lett. 17(22) , 6172-7, (2007)

Full Text: HTML

Abstract

A series of benzazepinones were synthesized and evaluated as hNa(v)1.7 sodium channel blockers. Several compounds from this series displayed good oral bioavailability and exposure and were efficacious in a rat model of neuropathic pain.