Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors.
نویسندگان
چکیده
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.
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ورودعنوان ژورنال:
- Bioorganic & medicinal chemistry letters
دوره 20 4 شماره
صفحات -
تاریخ انتشار 2010