Ultra-short-acting .beta.-adrenergic receptor blocking agents. 3. Ethylenediamine derivatives of (aryloxy)propanolamines having esters on the aryl function

Abstract

Various ethylenediamine derivatives were incorporated into the N substituent of certain short-acting (aryloxy)propanolamine systems that contain esters on their aryl functions. Although several of these compounds showed durations of action comparable to their prototypes, most of the N substituents significantly prolonged the duration of .beta.-adrenergic blockade. While 1 of the compounds showed appreciable cardioselectivity in vitro [in guinea pig preparations], generally little enhancement of cardioselectivity was obtained. A brief discussion of structure-activity relationships observed for the ethylenediamine derivatives is presented.