Key result
Novel phenylimidazole derivatives demonstrate potent cardioselective beta-blockade and acute antihypertensive activity.
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Modification of the pharmacological profile of the vasodilating/beta-adrenergic blocking agent 2-[4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl]-4-(trifluoromethyl)imidazole (1) has been investigated. Introduction of selected substitutents onto the imidazole ring, in place of the trifluoromethyl group, has yielded highly cardioselective beta-adrenergic blocking agents such as 7, 17, and 18. The placement of alkyl or chloro groups onto the aryl ring of 1, as illustrated by 33, has produced a class of compounds characterized as antihypertensive beta-adrenergic blocking agents. In these examples, the acute antihypertensive activity does not appear to be due to either vasodilating or beta 2-agonist properties.
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Baldwin et al. (1979) studied Hypertension. 2-[4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl]-4-(trifluoromethyl)imidazole (1) derivatives (e.g., compounds 7, 17, 18, 33) was evaluated on Cardioselectivity and acute antihypertensive activity. Modified 2-[4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl]imidazole derivatives (e.g., 7, 17, 18, 33) yielded cardioselective and acute antihypertensive beta-blockers.
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