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 compounds 5 and 21 exhibited both anti-allodynic and anti-hyperalgesic activity in the spinal nerve ligation model of neuropathic pain.

Citation

Pajouhesh, H., Feng, Z. P., Ding, Y., Zhang, L., Pajouhesh, H., Morrison, J. L., … Snutch, T. P. (2010). Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors. Bioorganic and Medicinal Chemistry Letters, 20(4), 1378–1383. https://doi.org/10.1016/j.bmcl.2010.01.008

URI

http://hdl.handle.net/1880/106672

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