Potent nonpeptide endothelin antagonists:: Synthesis and structure-activity relationships of pyrazole-5-carboxylic acids

被引：29
|
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 / 22期
关键词：
D O I：
10.1016/S0960-894X(00)00513-8
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
We have previously reported the identification of pyrazole-5-carboxylic acids as a new class of endothelin antagonists from low affinity pyrazol-5-ol ligands, which were obtained by random screening assays.(1) We describe herein the synthesis and the structure-activity relationships (SARs) of these pyrazole-5-carboxylic acids with potent ETA selective, mixed ETA/ETB or moderately ETB selective antagonist activities. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：2575 / 2578
页数：4
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