某些2,7-二（N-环氨基）-3-苯基-1,8-萘啶衍生物的合成及抗血小板活性

Synthesis and antiplatelet activity of some 2,7-di(N-cycloamino)-3-phenyl-1,8-naphthyridine derivatives.

作者信息

Ferrarini P L, Badawneh M, Franconi F, Manera C, Miceli M, Mori C, Saccomanni G

机构信息

Dipartimento di Scienze Farmaceutiche, Università di Pisa, Italy.

出版信息

Farmaco. 2001 Apr;56(4):311-8. doi: 10.1016/s0014-827x(01)01075-8.

DOI:10.1016/s0014-827x(01)01075-8

PMID:11421260

Abstract

Several 2,7-di(N-cycloamino)-3-phenyl-1,8-naphthyridine derivatives were synthesized and tested for their ability to inhibit human platelet aggregation in vitro induced by arachidonic acid, collagen and ADP. Only five compounds showed any appreciable activity, and the results of all the active derivatives were similar to those of papaverine in the test with arachidonic acid and collagen. Moreover, the most active compounds were investigated in the test with ADP and again showed a significant activity. The tested compounds that possessed the best activity were also shown to increase the c-AMP level significantly without involving the adenylyl cyclase system.

摘要

合成了几种2,7-二（N-环氨基）-3-苯基-1,8-萘啶衍生物，并测试了它们在体外抑制花生四烯酸、胶原蛋白和ADP诱导的人血小板聚集的能力。只有五种化合物表现出任何明显的活性，并且所有活性衍生物在花生四烯酸和胶原蛋白测试中的结果与罂粟碱相似。此外，对活性最强的化合物进行了ADP测试，结果再次显示出显著活性。具有最佳活性的测试化合物还显示出能显著提高c-AMP水平，且不涉及腺苷酸环化酶系统。