Document Report Card

ID: ALA1122388

Journal: J Med Chem

Title: beta 1-selective adrenoceptor antagonists. 2. 4-ether-linked phenoxypropanolamines.

Authors: Machin PJ, Hurst DN, Bradshaw RM, Blaber LC, Burden DT, Fryer AD, Melarange RA, Shivdasani C.

Abstract: A series of 4-substituted phenoxypropanolamines was prepared and examined for beta-adrenoceptor activity. Some of the compounds, especially the [4-[2-[[2-(4-fluorophenyl)ethyl] oxy]ethoxy]phenoxy]propanolamines (14, 15, and 24), showed potent beta 1-blockade with virtually no beta 2-blockade at doses over a 1000 times greater. The compounds also possessed partial agonist activity. Structure-activity relationships are discussed, and conclusions are drawn about the binding sites on beta-adrenoceptors.

CiteXplore: 6138435

DOI: 10.1021/jm00365a005