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

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

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Citation Number: 65

Abstract

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 ( ...