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

页码：915 / 918

页数：4

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