1,4-diaryl-2-oxo-1,2-dihyrdo-quinoline-3-carboxylic acids as endothelin receptor antagonists

被引:43
作者
Mederski, WWKR
Osswald, M
Dorsch, D
Christadler, M
Schmitges, CJ
Wilm, C
机构
[1] Merck KGaA, Preclinical Pharmaceutical Research
关键词
D O I
10.1016/S0960-894X(97)00319-3
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 1,4-diaryl-2-oxo-1,2-dihydro-quinoline-3-carboxylic acids as non-selective endothelin ETA/ETB receptor antagonists are described. The most potent inhibitor 3m displayed an IC50 of 260 nM and 200 nM for ETA and ETB receptors,respectively. (C) 1997 Elsevier Science Ltd.
引用
收藏
页码:1883 / 1886
页数:4
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