Synthesis and platelet aggregation inhibitory effects of N-[(1H-pyrazol-1-yl)alkyl]benzoylamides.

A series of N-[(1H-pyrazol-1-yl)alkyl]benzoylamides was synthesized and tested in vitro for their inhibitory effects on adenosine diphosphate-, collagen-, arachidonic acid- and thrombin-induced aggregation of human platelets. Among them, N-[(1H-pyrazol-1-yl)butyl]benzoylamide (Ve) was found to have the most potent inhibitory activity. The structure-activity relationships are reported. The biological activity of the title compounds is reported in parallel with that of a known inhibitor of thromboxane A2 synthetase.