Antiaggregatory activity of imidazoline drugs and chemicals as a function of their structure.

The concentration-response curves were constructed for 18 azole derivatives (including seven imidazoline drugs) as the inhibitors of the adrenaline-induced human blood platelet aggregation. It was demonstrated by the quantitative structure-activity relationships analysis that the less hydrophobic agents started to act as effective inhibitors at lower concentrations but that stronger effects could be obtained with the more hydrophobic derivatives. The conclusion was drawn that the inhibitory activity observed was the result of nonspecific hydrophobic interactions of the agents with both an andrenergic platelet receptor and a site of loss on serum albumin.