An interdisciplinary approach to the design of new structures active at the .beta.-adrenergic receptor. Aliphatic oxime ether derivatives
- 31 January 1985
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 28 (2) , 153-160
- https://doi.org/10.1021/jm00380a001
Abstract
On the basis of results previously obtained from structural and theoretical studies on .beta.-adrenergic drugs, a series of aliphatic oxime ether derivatives (AOED) was synthesized. Pharmacological in vitro tests showed that the compounds exhibited a marked and competitive antagonism at rat and guinea pig .beta.-adrenoceptors; the .beta.2/.beta.1 selectivity ratio indicated that they were more active on the tracheal than on the cardiac .beta.-receptor. The chemical reactivity of the AOED was studied through the calculation of the electrostatic molecular potential (EMP) on a model compound in its preferred conformation. The EMP trend agreed with that previously calculated for other .beta.-blocking drugs.This publication has 13 references indexed in Scilit:
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