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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Doherty GA,Bhatia P,Vortherms TA,Marsh KC,Wetter JM,Mack H,Scott VE,Jarvis MF,Stewart AO

doi

10.1016/j.bmcl.2011.12.100

subject

Has Abstract

pub_date

2012-02-15 00:00:00

pages

1716-8

issue

4

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)01782-3

journal_volume

22

pub_type

杂志文章

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