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


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… (More)
DOI: 10.1016/j.bmcl.2010.01.008


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