Hou G, Gravier D, Casadebaig F, Dupin J P, Bernard H, Boisseau M
Laboratoire de Chimie Organique, Université de Bordeaux II, France.
Pharmazie. 1995 Nov;50(11):719-22.
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.
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。
