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A series of 2-(arylamino)imidazoles was synthesized and evaluated for activity at alpha1- and alpha2-adrenoceptors. This class of agents has been shown to have potent and selective agonist activity at the alpha2-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.
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