Amidinosemicarbazido derivatives of pyrazole: synthesis and inhibitory effect on blood coagulation and platelet aggregation.
Amidinosemicarbazido derivatives of pyrazole having various substituents on pyrazole ring were prepared and their effect on platelet function and blood coagulation was determined in vitro. Platelet aggregation and serotonin release induced by ADP, collagen, arachidonic acid and thrombin were markedly inhibited by pyrazole derivatives at mM concentrations. Compounds with a hydrophobic nucleus at position 1 of the pyrazole ring showed the most potent antiplatelet activity. On the contrary, their effect on blood coagulation was faintly inhibitory.
Ferroni
R
R
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy.
Milani
L
L
Simoni
D
D
Orlandini
P
P
Poli
T
T
Guarneri
M
M
Taddeo
U
U
D000925:Anticoagulants / Q000138:chemical synthesis*; D006801:Humans; D010314:Partial Thromboplastin Time; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis*; D011517:Prothrombin Time; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000925:Anticoagulants; D010975:Platelet Aggregation Inhibitors; D011720:Pyrazoles