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

Bioorganic & Medicinal Chemistry Letters
2012.0

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.

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