Optically active derivatives of imidazolines. .alpha.-Adrenergic blocking properties

Abstract
The synthesis and .alpha.-adrenergic blocking activity of a series of optically active 2,4-disubstituted imidazolines are presented. The substituted analogs of naphazoline, tolazoline and clonidine possess moderate .alpha.-adrenergic blocking activity with -log KB values in the range from 4.77-6.57. The differences between the .alpha.-adrenergic blocking activity of the stereoisomers of the 2,4-disubstituted imidazolines were small or insignificant in the rabbit aortic tissue preparations.