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.

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页码：2575 / 2578

页数：4

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