Discovery of diphenyl lactam derivatives as N-type calcium channel blockers

GA Doherty, P Bhatia, TA Vortherms, KC Marsh…

Index: Doherty, George A.; Bhatia, Pramila; Vortherms, Timothy A.; Marsh, Kennan C.; Wetter, Jill M.; MacK, Helmut; Scott, Victoria E.; Jarvis, Michael F.; Stewart, Andrew O. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 4 p. 1716 - 1718

Full Text: HTML

Citation Number: 9

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.