Benzofuro[3,2-b]pyridines as mixed ETA/ETB and selective ETB endothelin receptor antagonists

被引：34

作者：

Mederski, WWKR ^{[1
]}

Osswald, M ^{[1
]}

Dorsch, D ^{[1
]}

Christadler, M ^{[1
]}

Schmitges, CJ ^{[1
]}

Wilm, C ^{[1
]}

机构：

[1] Merck KGaA, Preclin Pharmaceut Res, D-64271 Darmstadt, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 04期

关键词：

antagonists; benzofuro[3,2-b]pyridines; endothelin; vasodilators;

D O I：

10.1016/S0960-894X(99)00040-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The discovery, synthesis and structure-activity relationships of a series of novel benzofuro[3,2-b]pyridines as non-selective endothelin ETA/ETB as well as selective ETB receptor antagonists are described. The most potent non-selective inhibitor 7s displayed an IC50 of 21 nM and 41 nM for ETA and ETB receptors, respectively, whereas 7ee merely showed affinity for the ETB receptor (IC50 = 3.6 nM). (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：619 / 622

页数：4

共 13 条

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