Pyridazinones with a pendant acylsulfonamide moiety as endothelin receptor antagonists

被引：13

作者：

Dorsch, D

Mederski, WWKR

Osswald, M

Devant, RM

Schmitges, CJ

Christadler, M

Wilm, C

机构：

[1] Merck KGaA, Preclinical Pharmaceutical Research

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 03期

关键词：

D O I：

10.1016/S0960-894X(96)00617-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Highly active endothelin receptor antagonists can be obtained by replacing the aryloxy group of L-749,329 by diversely substituted pyridazinone residues. The syntheses and structure-activity relationships of the new aryl-oxopyridazinyl-N-(4-arylsulfonyl)-acetamides 2 are reported. 2p with a simple dimethylpyridazinone moiety was one of the most potent compounds in vitro. (C) 1997, Elsevier Science Ltd.

引用

页码：275 / 280

页数：6

共 20 条

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