Optimization of retro-thiorphan for inhibition of endothelin converting enzyme

被引：10
作者：
Kukkola, PJ
Bilci, NA
Kozak, WX
Savage, P
Jeng, AY
机构：
[1] Research Department, Pharmaceuticals Division, CIBA-GEIGY Corporation, Summit
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 06期
关键词：
D O I：
10.1016/0960-894X(96)00091-1
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The structural requirements of retro-thiorphan, N-[1R,S-benzyl-2-mercaptoethyl]malonamic acid 2, analogs for the inhibition of endothelin converting enzyme (ECE) were investigated. Although based on a single amino acid residue, N-[1R-(1H-indol-3-ylmethyl)-2-mercaptoethyl]-2-phenylacetamide 28 was found to be two times more potent than the widely utilized reference inhibitor phosphoramidon.
引用
收藏
页码：619 / 624
页数：6
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