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

✍ Scribed by Ragab M. Shafik; Abdel-Fattah A. A. Askar

• Publisher: John Wiley and Sons
• Year: 1979
• Tongue: English
• Weight: 567 KB
• Volume: 68
• Category: Article
• ISSN: 0022-3549
• DOI: 10.1002/jps.2600680629

✦ Synopsis

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.