Rutaecarpine衍生物的合成及体外抗血小板聚集活性

Synthesis and anti-platelet aggregation activities in vitro of rutaecarpine derivatives

目的合成新的rutaecarpine衍生物并对其抗血小板聚集活性进行研究。方法先合成rutaecarpine,再进行N-取代反应,合成目标化合物,并测试所合成化合物的体外抗血小板聚集活性。结果与结论共合成6个未见文献报道的新化合物,它们的结构经1H-NMR和MS确证。初步体外药理实验结果显示:有4个新化合物对血小板聚集的抑制作用强于母体化合物rutaecarpine。

Aim To design and synthesize new rutaecarpine derivatives, and to evaluate their activities of antiplatelet aggregation. Methods Rutaecarpine was prepared, then the target compounds were synthesized from rutaecarpine via N-substitution. Their anti-platelet aggregation activities were determined in vitro. Results and conclusions Six derivatives of rutaecarpine were synthesized with the structures confirmed by their ^1H- NMR and MS spectra. The primary pharmacological test in vitro shows that the anti-platelet aggregation activities of four new derivatives are higher than that of rutaecarpine.