Structure-activity relationship of N-methyl-N-aralkyl-peptidylamines as novel N-type calcium channel blockers

被引：19
|
作者：
Hu, LY
Ryder, TR
Rafferty, MF
Dooley, DJ
Geer, JJ
Lotarski, SM
Miljanich, GP
Millerman, E
Rock, DM
Stoehr, SJ
Szoke, BG
Taylor, CP
Vartanian, MG
机构：
[1] Parke Davis Pharmaceut Res, Ann Arbor, MI 48105 USA
[2] Elan Pharmaceut Inc, Menlo Park, CA 94025 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 15期
关键词：
D O I：
10.1016/S0960-894X(99)00359-5
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Selective N-type voltage sensitive calcium channel (VSCC) blockers have shown efficacy in several animal models of stroke and pain. In the process of searching for small molecule N-type calcium channel blockers, we have identified a series of N-methyl-N-aralkyl-peptidylamines with potent functional activity at N-type VSCCs. The most active compound discovered in this series is PD 173212 (11, IC50 = 36 nM in the IMR-32 assays). SAR and pharmacological evaluation of this series are described, (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：2151 / 2156
页数：6
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