- Benzazepinone Nav1.7 blockers: potential treatments for neuropathic pain.
Benzazepinone Nav1.7 blockers: potential treatments for neuropathic pain.
Bioorganic & medicinal chemistry letters (2007-09-25)
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
PMID17889534
摘要
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.