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.
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.
D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis*; D000818:Animals; D001001:Anura; D001713:Biphenyl Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects; D004285:Dogs; D004336:Drug Antagonism; D006321:Heart / Q000187:drug effects; D066298:In Vitro Techniques; D013329:Structure-Activity Relationship
D000319:Adrenergic beta-Antagonists; D001713:Biphenyl Compounds