Synthesis and beta-adrenergic blocking activity of new aliphatic oxime ethers.

Basic Information

ID: ALA1121606

Journal: J Med Chem

Title: Synthesis and beta-adrenergic blocking activity of new aliphatic oxime ethers.

Authors: Leclerc G, Bieth N, Schwartz J.

Abstract: New beta-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 (beta 2/beta 1 ratio approximately 15). The role and importance of the aromatic nucleus in this class of compounds are discussed.

CiteXplore: 6104730

DOI: 10.1021/jm00180a007

Patent ID: