Synthesis and .beta.-adrenergic blocking activity of a novel class of aromatic oxime ethers
- 1 December 1977
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 20 (12) , 1657-1662
- https://doi.org/10.1021/jm00222a023
Abstract
A new series of .beta.-adrenergic blocking amines containing an oximino-propanolic chain linked to an aromatic nucleus was synthesized. Most of the derivatives are characterized by .beta.2-selectivity. The structure-activity relationships are discussed. One of the compounds, selected for further studies, was more active on the trachea than on the atria of guinea pig, 155 times in vitro and 26 times in vivo. Butoxamine''s .beta.2-selectivity is 13 in vitro and only 2 in vivo. With a series of 30 acetophenone oxime derivatives, no quantitative structure-activity relationships could be detected.This publication has 2 references indexed in Scilit:
- Clonidine and related analogues. Quantitative correlationsJournal of Medicinal Chemistry, 1976
- New series of cardioselective adrenergic .beta.-receptor blocking compounds. 1-(2-Acyl-4-acylaminophenoxy)-3-isopropylaminopropan-2-olsJournal of Medicinal Chemistry, 1976