Cardioselective beta-adrenergic blocking agents. 1. 1-((3,4-Dimethoxyphenethyl)amino)-3-aryloxy-2-propanols.
J Med Chem, 1975/2;18(2):148-52.
Hoefle ML, Hastings SG, Meyer RF, Corey RM, Holmes A, Stratton CD
PMID: 235644
Impact factor: 8.039
Abstract
A series of 1-amino-3-aryloxy-2-propanols has been synthesized and examined for cardioselective beta-blockade. The introduction of the (3,4-dimethoxyphenethyl)amino group lead to the most cardioselective agents. Structure-activity relationships are discussed. Of the compounds tested 1-[(3,4-dimethoxyphenethyl)amino]-3-(m-tolyloxy)-2-propanol was selected for clinical trial because of optimal potency and selectivity.
MeSH terms
Adrenergic beta-Antagonists; Animals; Dose-Response Relationship, Drug; Guinea Pigs; Heart; Heart Atria; Heart Rate; In Vitro Techniques; Isoproterenol; Muscle Contraction; Phenethylamines; Propanolamines; Structure-Activity Relationship; Trachea
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