Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists

被引：113

作者：

Riechers, H ^{[1
]}

Albrecht, HP ^{[1
]}

Amberg, W ^{[1
]}

Baumann, E ^{[1
]}

Bernard, H ^{[1
]}

Bohm, HJ ^{[1
]}

Klinge, D ^{[1
]}

Kling, A ^{[1
]}

Muller, S ^{[1
]}

Raschack, M ^{[1
]}

Unger, L ^{[1
]}

Walker, N ^{[1
]}

Wernet, W ^{[1
]}

机构：

[1] KNOLL AG,D-67008 LUDWIGSHAFEN,GERMANY

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1996年 / 39卷 / 11期

关键词：

D O I：

10.1021/jm960274q

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel class of endothelin-A receptor ligands was discovered by high-throughput screening. Lead structure optimization led to highly potent antagonists which can be synthesized in a short sequence. The compounds are endothelin-A-selective, are orally available, and show a long duration of action.

引用

页码：2123 / 2128

页数：6

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