New β-adrenoceptor-blocking agents derived from dicyclopropyl ketone oxime: influence of amino substituents on in vivo activity

A Charaf, M Bouzoubaa, A Bouzoubaa, M Blanc…

Index: Charaf; Bouzoubaa; Blanc; Leclerc European Journal of Medicinal Chemistry, 1994 , vol. 29, # 1 p. 69 - 74

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Citation Number: 5

Abstract

Abstract A series of oximinopropanolamines derived from dicyclopropyl ketone, in which the amine substituents were alkyl, cycloalkyl, aryl and aralkyl groups, has been synthesized. The β-adrenergic blocking properties were determined on anaesthetized rats. Two N-aralkyl derivatives were found to be as potent as propranolol and compound 11 was twice as active as propranolol. Some structure-activity relationships are discussed.