- Discovery of diphenyl lactam derivatives as N-type calcium channel blockers.
Discovery of diphenyl lactam derivatives as N-type calcium channel blockers.
Bioorganic & medicinal chemistry letters (2012-01-27)
George A Doherty, Pramila Bhatia, Timothy A Vortherms, Kennan C Marsh, Jill M Wetter, Helmut Mack, Victoria E Scott, Michael F Jarvis, Andrew O Stewart
PMID22277280
ABSTRACT
A novel series of diphenyl lactam containing calcium channel blockers is described. Extensive SAR studies resulted in compounds with low molar activity and good plasma exposure after oral dosing. Compounds 2, 6 and 7 demonstrated significant efficacy in the capsaicin model of secondary hyperalgesia following oral administration.
MATERIALS