beta-adrenergic blocking agents. 24. Heterocyclic substituted 1-(aryloxy)-3-[[(amido)alkyl]amino]propan-2-ols.
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.
D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis*; D000818:Animals; D002415:Cats; D055598:Chemical Phenomena; D002621:Chemistry; D004305:Dose-Response Relationship, Drug; D006339:Heart Rate / Q000187:drug effects; D011412:Propanolamines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats
D000319:Adrenergic beta-Antagonists; D011412:Propanolamines