2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series

A series of 2'-heteroaryl and 2'-oxime anilinomethylimidazolines was prepared and evaluated in in vitro functional assays for cloned human alpha1A, alpha1B, and alpha1D receptor subtypes. Potent and selective alpha1A agonists have been identified in these series.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2002-02, Vol.12 (4), p.575-579
Main Authors: Navas, 3rd, Frank, Bishop, Michael J, Garrison, Deanna T, Hodson, Stephen J, Speake, Jason D, Bigham, Eric C, Drewry, David H, Saussy, David L, Liacos, James H, Irving, Paul E, Gobel, M Jeffrey
Format: Article
Language:English
Subjects:
Adrenergic alpha-1 Receptor Agonists
Adrenergic alpha-Agonists - chemical synthesis
Adrenergic alpha-Agonists - chemistry
Adrenergic alpha-Agonists - pharmacology
Animals
Calcium Signaling - drug effects
Cell Line
Cloning, Molecular
Heterocyclic Compounds
Humans
Imidazoles - chemical synthesis
Imidazoles - chemistry
Imidazoles - pharmacology
Oximes
Phenylephrine - metabolism
Protein Binding
Rats
Receptors, Adrenergic, alpha-1 - metabolism
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Description
Summary:A series of 2'-heteroaryl and 2'-oxime anilinomethylimidazolines was prepared and evaluated in in vitro functional assays for cloned human alpha1A, alpha1B, and alpha1D receptor subtypes. Potent and selective alpha1A agonists have been identified in these series.
ISSN:0960-894X