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Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors.

Abstract：

:A novel series of compounds derived from the previously reported N-type calcium channel blocker NP118809 (1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one) is described. Extensive SAR studies resulted in compounds with IC(50) values in the range of 10-150 nM and selectivity over the L-type channels up to nearly 1200-fold. Orally administered compounds 5 and 21 exhibited both anti-allodynic and anti-hyperalgesic activity in the spinal nerve ligation model of neuropathic pain.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Pajouhesh H,Feng ZP,Ding Y,Zhang L,Pajouhesh H,Morrison JL,Belardetti F,Tringham E,Simonson E,Vanderah TW,Porreca F,Zamponi GW,Mitscher LA,Snutch TP

doi

10.1016/j.bmcl.2010.01.008

subject

Has Abstract

pub_date

2010-02-15 00:00:00

pages

1378-83

issue

4

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00010-7

journal_volume

20

pub_type

杂志文章

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