Syntheses and β-Adrenergic Blocking Activities of Carbostyril Derivatives

Abstract

Many 5-(3-amino-2-hydroxypropoxy)-8-alkoxy and acyloxy-3, 4-dihydrocarbostyrils and 5-(3-amino-2-hydroxypropoxy)-8-alkoxycarbostyrils were synthesized from 5, 8-dihydroxy-3, 4-dihydrocarbostyril, and their β-adrenergic blocking activities were examincd. Among them, 8-acetonyloxy-5-[3-(3, 4-dimethoxyphenethylamino)-2-hydroxypropoxy]-3, 4-dihydrocarbostyril hydrochloride hydrate (IVh) was found to have potent β₁-selective adrenergic blocking activity.