Structure-activity study of L-cysteine-based N-type calcium channel blockers: Optimization of N- and C-terminal substituents

被引：18
|
作者：
Seko, T [1 ]
Kato, M [1 ]
Kohno, H [1 ]
Ono, S [1 ]
Hashimura, K [1 ]
Takimizu, H [1 ]
Nakai, K [1 ]
Maegawa, H [1 ]
Katsube, N [1 ]
Toda, M [1 ]
机构：
[1] Ono Pharmaceut Co Ltd, Minase Res Inst, Osaka 6188585, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 06期
关键词：
D O I：
10.1016/S0960-894X(02)00032-X
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Synthesis and structure-activity relationship (SAR) studies of L-cysteine-based N-type calcium channel blockers are described. In the course of exploring SAR of the N- and C-terminal substituents, the L-cysteine derivative 4b was found to be a potent N-type calcium channel blocker with an IC50 value of 0.14 muM on IMR-32 assay. Compound 4b showed 12-fold selectivity for N-type over L-type calcium channels on AtT-20 assay. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：915 / 918
页数：4
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