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吡啶并[2,3 - d]嘧啶 - 4(3H) - 酮衍生物和1,2,3,4 - 四氢吡啶并[2,3 - d]嘧啶衍生物:合成及其抗血小板聚集活性的体外研究

Pyrido[2,3-d]pyrimidin-4(3H)-one derivatives and 1,2,3,4-tetrahydro- pyrido[2,3-d]pyrimidine derivatives: synthesis and in vitro study of their activity against platelet aggregation.

作者信息

Hou G, Gravier D, Casadebaig F, Dupin J P, Bernard H, Boisseau M

机构信息

Laboratoire de Chimie Organique, Université de Bordeaux II, France.

出版信息

Pharmazie. 1995 Nov;50(11):719-22.

PMID:8570668
Abstract

Some new derivatives of pyrido[2,3-d]pyrimidin-4(3H)-one A and 1,2,3,4-tetrahydro-pyrido[2,3-d]pyrimidines B were prepared. The study of their in vitro antiaggregating activity showed that the compounds A possessed an inhibitory potency when aggregation was induced with ADP. Their reduction to derivatives of 1,2,3,4-tetrahydro-pyrido[2,3-d]pyrimidine B led to a new series of molecules possessing a greater antiaggregating power. When compared to that of acetylsalicylic acid under the same conditions, this activity was weaker with collagen, the same with arachidonic acid-induced aggregation, but greater when aggregation was induced by ADP. However, they inhibited serotonin release only slightly. Compared to ginkgolide they remained weaker with PAF-induced aggregation.

摘要

制备了一些吡啶并[2,3 - d]嘧啶 - 4(3H)-酮A和1,2,3,4 - 四氢吡啶并[2,3 - d]嘧啶B的新衍生物。对它们体外抗聚集活性的研究表明,当用ADP诱导聚集时,化合物A具有抑制效力。将它们还原为1,2,3,4 - 四氢吡啶并[2,3 - d]嘧啶B的衍生物产生了一系列具有更强抗聚集能力的新分子。在相同条件下与乙酰水杨酸相比,它们对胶原蛋白诱导的聚集活性较弱,对花生四烯酸诱导的聚集活性相同,但对ADP诱导的聚集活性更强。然而,它们仅轻微抑制血清素释放。与银杏内酯相比,它们对PAF诱导的聚集活性仍然较弱。

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