2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: alpha1a subtype selective 2'-heteroaryl compounds |
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| Authors: | Speake Jason D Navas Frank Bishop Michael J Garrison Deanna T Bigham Eric C Hodson Stephen J Saussy David L Liacos Jim A Irving Paul E Sherman Bryan W |
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| Institution: | GlaxoSmithKline, 5Moore Drive, Research Triangle Park, NC 27709, USA. jason.d.speake@gsk.com |
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| 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. |
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