川芎哚的结构改造及生物活性研究

STRUCTURAL MODIFICATION AND BIOACTIVITY OF PERLOLYRINE

摘要: 目的:寻找新型的心血管药物。方法:根据推理药物设计原理,设计合成目标化合物,并研究其生物活性。结果:合成了16个川芎哚的类似物(I～XVI),其中8个化合物(I,I,V～VI,IX,XI和XV)是新化合物。结论:所合成的川芎哚类似物均有一定程度的抗血小板聚集作用,其中I～IV,VI,X,XI及XII有一定程度的抗血栓作用。

Abstract: AIM: To search for compounds for the treatment of cardiovascular diseases. METHODS: According to rational drug design principle, a series of analogues of perlolyrine were prepared, and the antiplatelet aggregation activity and antithrombotic effects of these compounds were tested. RESULTS: Sixteen perlolyrine analogues were synthsized(I～XVI). Of them, 8 compounds(I,II,V～VII,IX,XI and XV) were first reported. CONCLUSION: All synthesized compounds showed antiplatelet aggregation activity to a certain degree. Of them, 8 compounds(I～IV,VII,X,XI and XIII) exhibited antithrombotic effects.