Optically active derivatives of imidazolines. alpha-Adrenergic blocking properties.
The synthesis and alpha-adrenergic blocking activity of a series of optically active 2,4-disubstituted imidazolines are presented. The substituted analogues of naphazoline, tolazoline, and clonidine possess moderate alpha-adrenergic blocking activity with -log KB values in the range from 4.77 to 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.
D000317:Adrenergic alpha-Antagonists / Q000138:chemical synthesis*; D000818:Animals; D001013:Aorta, Thoracic / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D009119:Muscle Contraction / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D011817:Rabbits; D013237:Stereoisomerism
D000317:Adrenergic alpha-Antagonists; D007093:Imidazoles