Synthesis and Evaluation of 2-(Arylamino)imidazoles as α2-Adrenergic Agonists

A series of 2-(arylamino)imidazoles was synthesized and evaluated for activity at α1- and α2-adrenoceptors. This class of agents has been shown to have potent and selective agonist activity at the α2-adrenoceptors. The most potent member of this class, 2-[(5-methyl-1,4-benzodioxan-6-yl)amino]imidazo...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1997-01, Vol.40 (1), p.18-23
Main Authors: Munk, Stephen A, Harcourt, Dale A, Arasasingham, Premilla N, Burke, James A, Kharlamb, Alexander B, Manlapaz, Cynthia A, Padillo, Edwin U, Roberts, Donald, Runde, Eileen, Williams, Linda, Wheeler, Larry A, Garst, Michael E
Format: Article
Language:English
Subjects:
Biological and medical sciences
Eye
Medical sciences
Pharmacology. Drug treatments
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Summary:A series of 2-(arylamino)imidazoles was synthesized and evaluated for activity at α1- and α2-adrenoceptors. This class of agents has been shown to have potent and selective agonist activity at the α2-adrenoceptors. The most potent member of this class, 2-[(5-methyl-1,4-benzodioxan-6-yl)amino]imidazole, proved efficacious for the reduction of intraocular pressure upon topical administration and for the reduction of blood pressure upon intravenous administration. During the course of our studies, we developed a new reagent that allowed rapid assembly of the target compounds. This reagent, N-(2,2-diethoxyethyl)carbodiimide, was convenient to prepare and was stable under low-temperature storage conditions.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm9605142