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

M J Bishop; J Berman; E C Bigham; D T Garrison; M J Gobel; S J Hodson; P E Irving; J A Liacos; D J Minick; F Navas; D L Saussy Jr; J D Speake

doi:10.1016/s0960-894x(01)00569-8

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

Bioorg Med Chem Lett. 2001 Nov 5;11(21):2871-4. doi: 10.1016/s0960-894x(01)00569-8.

Authors

M J Bishop¹, J Berman, E C Bigham, D T Garrison, M J Gobel, S J Hodson, P E Irving, J A Liacos, D J Minick, F Navas, D L Saussy Jr, J D Speake

Affiliation

¹ GlaxoSmithKline, 5Moore Drive, Research Triangle Park, NC 27709, USA. mjb45288@glaxowellcome.com

PMID: 11597419
DOI: 10.1016/s0960-894x(01)00569-8

Abstract

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.

MeSH terms

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

Substances

Adrenergic alpha-1 Receptor Agonists
Adrenergic alpha-Agonists
Amides
Carboxylic Acids
Esters
Imidazoles