Nondepressant beta-adrenergic blocking agents. 1. Substituted 3-amino-1-(5,6,7,8-tetrahydro-1-naphthoxy)-2-propanols.
A series of 3-amino-1-(5,6,7,8-tetrahydronaphthoxy)-2-propanols was synthesized and investigated for beta-adrenergic blocking activity and direct myocardial depressant action. The cis- and trans-diols 12--15 were found to retain the beta-blocking potency of propranolol but to lack its myocardial depressant action. Compound 15 (nadolol) is currently undergoing extensive clinical evaluation as a potential antianginal, antiarrhythmic, and antihypertensive agent.
D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D002415:Cats; D004852:Epoxy Compounds; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007545:Isoproterenol / Q000037:antagonists & inhibitors; D008722:Methods; D009200:Myocardial Contraction / Q000187:drug effects; D010636:Phenols; D011412:Propanolamines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship
D000319:Adrenergic beta-Antagonists; D004852:Epoxy Compounds; D010636:Phenols; D011412:Propanolamines; D007545:Isoproterenol