2-(anilinomethyl)imidazolines as α1 adrenergic receptor agonists:: α1a subtype selective 2′-heteroaryl compounds

被引:17
|
作者
Speake, JD [1 ]
Navas, F [1 ]
Bishop, MJ [1 ]
Garrison, DT [1 ]
Bigham, EC [1 ]
Hodson, SJ [1 ]
Saussy, DL [1 ]
Liacos, JA [1 ]
Irving, PE [1 ]
Sherman, BW [1 ]
机构
[1] GlaxoSmithKline, Res Triangle Pk, NC 27709 USA
关键词
D O I
10.1016/S0960-894X(03)00050-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The structure-activity relationship of 2'-pyrrole, pyrazole and triazole substituted 2-(anilinomethyl)imidazolines as alpha(1) adrenergic agonists was investigated. The size and orientation of substituents, as well as the position of the heteroatoms, were found to have a profound effect on the potency and selectivity of the molecules. Potent alpha(1A) subtype selective agonists have been identified. (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1183 / 1186
页数:4
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