Multiple parallel synthesis of N,N-dialkyldipeptidylamines as N-type calcium channel blockers

被引：18

作者：

Ryder, TR

Hu, LY

Rafferty, MF

Millerman, E

Szoke, BG

Tarczy-Hornoch, K

机构：

[1] Parke Davis Pharmaceut Res, Dept Chem, Ann Arbor, MI 48105 USA

[2] Elan Pharmaceut Inc, Menlo Park, CA 94025 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 13期

关键词：

D O I：

10.1016/S0960-894X(99)00284-X

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 and pain. A series of N,N-dialkyldipeptidylamines with potent functional activity at N-type VSCC's has been identified. Multiple parallel synthesis of a focused array of thirty compounds using polymer-supported quenching reagents and preliminary pharmacology are presented. Eighteen compounds were identified with an IC50 below 1 mu M in an in vitro functional assay. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：1813 / 1818

页数：6

共 8 条

[1] Polymer-supported quenching reagents for parallel purification [J].