2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides

2-(Anilinomethyl)imidazolines with 2'-esters or 2'-amides are potent agonists of the cloned human alpha(1)-adrenoceptors in vitro. The size and shape of the ortho substituent can have significant effects on the potency, efficacy, and subtype selectivity of these 2-(anilinomethyl)imidazolin...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2001-11, Vol.11 (21), p.2871-2874
Main Authors: Bishop, M J, Berman, J, Bigham, E C, Garrison, D T, Gobel, M J, Hodson, S J, Irving, P E, Liacos, J A, Minick, D J, Navas, F, Saussy, Jr, D L, Speake, J D
Format: Article
Language:English
Subjects:
Adrenergic alpha-1 Receptor Agonists
Adrenergic alpha-Agonists - chemistry
Adrenergic alpha-Agonists - pharmacology
Amides - chemistry
Carboxylic Acids - chemistry
Esters - chemistry
Imidazoles - chemistry
Imidazoles - pharmacology
Structure-Activity Relationship
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Summary:2-(Anilinomethyl)imidazolines with 2'-esters or 2'-amides are potent agonists of the cloned human alpha(1)-adrenoceptors in vitro. The size and shape of the ortho substituent can have significant effects on the potency, efficacy, and subtype selectivity of these 2-(anilinomethyl)imidazolines. alpha(1A)-subtype selective agonists have been identified.
ISSN:0960-894X
DOI:10.1016/S0960-894X(01)00569-8