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2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: alpha1a subtype selective 2'-heteroaryl
Jason D Speake1, Frank Navas, Michael J Bishop
1GlaxoSmithKline, 5Moore Drive, Research Triangle Park, NC 27709, USA. jason.d.speake@gsk.com
Bioorganic & Medicinal Chemistry Letters
|March 20, 2003
Abstract:
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.