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

页码：2151 / 2156

页数：6

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