N-methyl-2-[4-(2-methylpropyl)phenyl]-3-(3-methoxy-5-methylpyrazin-2-ylsulfamoyl)benzamide; One of a class of novel benzenesulphonamides which are orally-active, ETA-selective endothelin antagonists

被引：4
|
作者：
Mortlock, AA
Bath, C
Butlin, RJ
Heys, C
Hunt, SJ
Reid, AC
Sumner, NF
Tang, EK
Whiting, E
Wilson, C
Wright, ND
机构：
[1] ZENECA Pharmaceuticals, Macclesfield, Cheshire, SK10 4TG, Alderley Park
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 11期
关键词：
D O I：
10.1016/S0960-894X(97)00228-X
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of novel sulphonamides have been discovered which show high affinity and selectivity for the endothelin ETA receptor. N-Methyl-2-[4-(2-methylpropyl)phenyl]-3-(3-methoxy-5-methylpyrazin-2-yl-sulfamoyl)benzamide (18) is the most widely investigated compound and is a potent antagonist in vivo when dosed either i.v. or orally, and has prolonged oral duration of action. (C) 1997 Elsevier Science Ltd.
引用
收藏
页码：1399 / 1402
页数：4
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