Amidinosemicarbazido derivatives of pyrazole: synthesis and inhibitory effect on blood coagulation and platelet aggregation.

Il Farmaco; edizione scientifica Pub Date : 1988-11-01
R Ferroni, L Milani, D Simoni, P Orlandini, T Poli, M Guarneri, U Taddeo
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Abstract

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.

吡唑氨基氨基脲基衍生物的合成及其对凝血和血小板聚集的抑制作用。
制备了吡唑环上具有不同取代基的氨基氨基脲基吡唑衍生物,并测定了其体外对血小板功能和凝血功能的影响。吡唑衍生物在mM浓度下显著抑制ADP、胶原、花生四烯酸和凝血酶诱导的血小板聚集和血清素释放。在吡唑环1号位置具有疏水核的化合物显示出最有效的抗血小板活性。相反,它们对凝血的抑制作用微弱。
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