Nonpeptide endothelin antagonists:: From lower affinity pyrazol-5-ols to higher affinity pyrazole-5-carboxylic acids

被引：26
|
作者：
Zhang, JD
Didierlaurent, S
Fortin, M
Lefrançois, D
Uridat, E
Vevert, JP
机构：
[1] Hoechst Marion Roussel, Med Chem, F-93235 Romainville, France
[2] Hoechst Marion Roussel, Cent Res, F-93235 Romainville, France
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 12期
关键词：
D O I：
10.1016/S0960-894X(00)00232-8
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Random screening of compounds in endothelin receptor (ETA and ETB) binding assays led to the discovery of a new class of pyrazol-5-ol ligands. Characterization of structural features crucial for binding activities of these pyrazol-5-ols, by structure-activity-relationship (SAR) studies, allowed us to design a novel class of pyrazole-5-carboxylic acids as more potent ET antagonists. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：1351 / 1355
页数：5
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