N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers

被引：19
作者：
Hu, LY
Ryder, TR
Rafferty, MF
Cody, WL
Lotarski, SM
Miljanich, GP
Millerman, E
Rock, DM
Song, YT
Stoehr, SJ
Taylor, CP
Weber, ML
Szoke, BG
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 / 06期
关键词：
D O I：
10.1016/S0960-894X(99)00100-6
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 utility in several models of stroke amid pain. We are especially interested in small molecule N-type calcium channel blockers for therapeutic use. Herein, we report a series of N,N-dialkyl-dipeptidylamines with potent functional activity at N-type VSCCs and in vivo efficacy. The synthesis, SAR, and pharmacological evaluation of this series are discussed. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：907 / 912
页数：6
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