Synthesis and β-Adrenergic Blocking Activity of New Aliphatic Oxime Ethers

Article abstract of DOI:10.1021/jm00180a007

New β-adrenergic blocking agents, most of which do not contain an aromatic nucleus, were synthesized.They were derived either from alkylamino-aliphatic oxime ethers, or alkylamino-aliphatic ethers.Most active among these are O-<3-(tert-butylamino)-2-hydroxypropyl>acetoxime (8; trachea pA₂=7.65) and 1-isobutoxy-3-(tert-butylamino)-2-propanol (15, trachea pA₂=7.49), both of which displayed bronchoselectivity (β₂/β₁ ratio ca. 15).The role and importance of the aromatic nucleus in this class of compounds are discussed