beta-Adrenergic blocking agents. 18. 1-(Aryloxy)-3-(arylthioalkylamino)propan-2-ols and 1-substituted alkylthioamino-3-(aryloxy)propan-2-ols.
The synthesis is described of a seris of derivaties of 1-(aryloxy)-3-(arylthioalkylamiho)propan-2-ols and 1-(alkylthioamino)- and 1-(aralkylamino)-3-(aryloxy)propan-2-ols. These compounds were investigated for their beta-adrenoreceptor blocking properties and their selectivity of action for the cardiac beta1 receptor. The structure-activity relationships are discussed with particular reference to the effects of the sulfur, sulfoxide, and sulfone groups on beta-adrenoreceptor blocking potency and selectivity.
D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis*; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D002415:Cats; D006339:Heart Rate / Q000187:drug effects; D011412:Propanolamines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013440:Sulfides / Q000138:chemical synthesis / Q000494:pharmacology; D013450:Sulfones / Q000138:chemical synthesis / Q000494:pharmacology; D013454:Sulfoxides / Q000138:chemical synthesis / Q000494:pharmacology
D000319:Adrenergic beta-Antagonists; D011412:Propanolamines; D013440:Sulfides; D013450:Sulfones; D013454:Sulfoxides