Nondepressant beta-adrenergic blocking agents. 1. Substituted 3-amino-1-(5,6,7,8-tetrahydro-1-naphthoxy)-2-propanols.
J Med Chem, 1978/9;21(9):913-22.
Condon ME, Cimarusti CM, Fox R, Narayanan VL, Reid J, Sundeen JE, Hauck FP
PMID: 31485
Impact factor: 8.039
Abstract
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.
MeSH terms
Adrenergic beta-Antagonists; Animals; Cats; Epoxy Compounds; Guinea Pigs; In Vitro Techniques; Isoproterenol; Methods; Myocardial Contraction; Phenols; Propanolamines; Rats; Structure-Activity Relationship
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