【摘要】 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%。更多还原

【Abstract】 Eight novel tetrahydrothienopyridine derivatives(4a～4h,yield of 85.5%～91.3%) with piperazine 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,4c and 4e exhibited obvious platelet aggregation inhibition,75.9% and 67.4%,respectively.更多还原