PMID: 37319Jun 1, 1979

New biphenyl derivatives II: 1-(4-Biphenylyl)-1-hydroxy-2-aminoethanes and 1-(4-biphenylyl)-1-chloro-2-aminoethanes as potential beta-adrenoceptor blocking agents

Journal of Pharmaceutical Sciences
R M Shafik, A F Askar


Series of 1-(4-biphenylyl)-1-hydroxy-2-aminoethanes and 1-(4-biphenylyl)-1-chloro-2-aminoethanes were synthesized. Newly developed reaction conditions for aryl aminomethyl ketone reduction and reductive alkylation, using sodium borohydride, are described. The prepared compounds were examined for adrenergic blocking activity on an anesthetized dog blood pressure preparation and on isolated toad hearts. beta-Adrenergic blockade was investigated using isoproterenol as the agonist. The benzylamino and cyclohexylamino analogs exhibited marked beta-adrenoceptor blocking activity, for which the latter derivatives were more potent.

Related Concepts

Structure-Activity Relationship
Diastolic Blood Pressure
Biphenyl Compounds
Drug Antagonism
Canis familiaris
Adrenergic beta-Antagonists

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