Document Report Card

ID: ALA1130342

Journal: J Med Chem

Title: Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists.

Authors: Munk SA, Harcourt DA, Arasasingham PN, Burke JA, Kharlamb AB, Manlapaz CA, Padillo EU, Roberts D, Runde E, Williams L, Wheeler LA, Garst ME.

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

CiteXplore: 9016324

DOI: 10.1021/jm9605142