Syntheses and β-Adrenergic Blocking Activities of Carbostyril Derivatives

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-dimethoxy...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 1981/08/25, Vol.29(8), pp.2166-2181
Hauptverfasser:	TOMINAGA, MICHIAKI, TONE, HITOSHI, NAKAGAWA, KAZUYUKI, TAKADA, KAORUKO, HOSHINO, YO, WATANABE, KOZO
Format:	Artikel
Sprache:	eng
Schlagworte:	3, 4-dimethoxyphenethylamine Adrenergic beta-Antagonists - chemical synthesis Animals Dogs Guinea Pigs In Vitro Techniques Male Propanolamines - chemical synthesis Propanolamines - pharmacology Quinolines - chemical synthesis Quinolines - pharmacology
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Zusammenfassung:	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.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.29.2166