M. Large, L. H. Smith
Dec 1, 1982
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Influential Citations
13
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Quality indicators
Journal
Journal of medicinal chemistry
Abstract
The synthesis of a series of 1-(aryloxy)-3-[[(amido)alkyl]amino] propan-2-ols where either the aryl moiety is heterocyclic or the amidic group is substituted by a heterocyclic moiety is described. Several of the compounds were more potent than propranolol when given intravenously to anesthetized rats. In contrast to previous findings with beta-blockers based on heterocyclic moieties and with either an isopropylamino or tert-butylamino substituent on the side chain, several compounds proved to be cardioselective when further examined in anesthetized cats. The detailed structure-activity relationships shown by this series of compounds are discussed.