新型含哌嗪的噻吩并四氢吡啶衍生物的合成及其抗血小板聚集活性

Synthesis and Anti-platelet Aggregation Activities in vivo of Novel Tetrahydrothienopyridine Derivatives with Piperazine

运用生物电子等排及药物代谢原理,设计并合成了8个新型的含哌嗪的噻吩并四氢吡啶类衍生物(4a～4h),产率85.5%～91.3%,其结构经1H NMR和HR-MS表征。大鼠体内血小板聚集模型评价测试结果表明,4a～4h均有一定抗血小板聚集活性,其中4c和4e的活性明显优于阳性对照药噻氯匹定,抑制率分别为75.9%和67.4%。

Eight novel tetrahydrothienopyridine derivatives（4a- 4h, yield of 85.5% - 91.3% ） withpiperazine were designed and synthesized by bioisosterism and principles of drug metabolism. The structures were characterized by ^1H NMR and HRMS. The anti-platelet aggregation activities were evaluated by platelet aggregation inhibition tests in rats. The results showed that 4a -4h exhibited certain anti-platelet aggregation activities. Compared with the positive control ticlopidine, 4e and 4e exhibited obvious platelet aggregation inhibition, 75.9% and 67.4%, respectively.