Synthesis of a series of compounds related to betaxolol, a new. beta. 1-adrenoceptor antagonist with a pharmacological and pharmacokinetic profile optimized for the …

…, J Rousseau, FM Lefevre-Borg, IG Cavero

文献索引：Manoury; Binet; Rousseau; Lefevre-Borg; Cavero Journal of Medicinal Chemistry, 1987 , vol. 30, # 6 p. 1003 - 1011

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被引用次数: 65

摘要

A series of para-substituted phenoxypropanolamines has been synthesized and tested for 0- adrenoceptor blocking activity. Some derivatives (8, 11, 12, 20, 21) exhibited greater in vitro potency than the reference drugs metoprolol and propranolol. This series, in contrast to propranolol but similar to metoprolol, possesses cardioselectivity. The 3-[p- [(cycloalkylmethoxy~ ethyl] phenoxy]-l-substituted-amino-2-propanol derivatives 8 ( ...