Syntheses and .BETA.-adrenergic blocking activities of carbostyril derivatives.

Publisher Website
Google Scholar
Abstract
Many compounds have been synthesized as candidates for the medical treatment of human angina pectoris, arrythmia and hypertension. 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 .beta.-adrenergic blocking activities were examined in guinea pigs and dogs. Among them, 8-acetonyloxy-5-[3-(3,4-dimethoxyphenethylamino)-2-hydroxypropoxy]-3,4-dihydrocarbostyril hydrochloride hydrate (IVh) has potent .beta.1-selective adrenergic blocking activity.