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.
Ferroni
R
R
Dipartimento di Scienze Farmaceutiche, Universitá di Ferrara, Italy.
Milani
L
L
Simoni
D
D
Orlandini
P
P
Bottura
M
M
Bardi
A
A
Guarneri
M
M
D055598:Chemical Phenomena; D002621:Chemistry; D006801:Humans; D066298:In Vitro Techniques; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship
D010975:Platelet Aggregation Inhibitors