Ferroni R, Milani L, Simoni D, Orlandini P, Bottura M, Bardi A, Guarneri M
Dipartimento di Scienze Farmaceutiche, Universitá di Ferrara, Italy.
Arzneimittelforschung. 1990 Jun;40(6):705-9.
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.
合成了一系列N-[(1H-吡唑-1-基)烷基]苯甲酰胺，并在体外测试了它们对二磷酸腺苷、胶原、花生四烯酸和凝血酶诱导的人血小板聚集的抑制作用。其中，N-[(1H-吡唑-1-基)丁基]苯甲酰胺（Ve）被发现具有最有效的抑制活性。报道了构效关系。同时报道了标题化合物与一种已知的血栓素A2合成酶抑制剂的生物活性。
