摘要
以达比加群酯为代表的Ⅱa因子抑制剂和以利伐沙班为代表的Xa因子抑制剂在抗凝血药物中起到了重要作用。本文综述了已上市的新型小分子抗凝血药物的的合成、作用机制及其构效关系,并对其进行了深入分析,同时对此类药物的发展趋势和前景进行了展望。
With the further research on the mechanism of coagulation and thrombosis,the pathogenesis of venous embolism and traditional drugs such as heparin and warfarin,Ⅱa factor and Xa factor in small molecules as the targets for new anticlotting drug played an important role in the new anticoagulant drugs.Among them,theⅡa factor inhibitors represented by dabigatran etexilate and the Xa factor inhibitor represented by rivaroxaban as two important antithrombotic drugs have become the hot topics in the study of medicinal chemists.This paper reviews the synthesis,action mechanism and structure-activity relationship of new small molecule anticoagulant drugs.The development trend and research prospect of this kind of drug are also prospected.
作者
李梦瑶
蔡志强
侯玲
李帅
LI Meng-yao;CAI Zhi-qiang;HOU Ling;LI Shuai(Liaoning Province Engineering Research Center for Fine Chemical Engineering of Aromatics Downstream,School of Petrochemical Engineering,Shenyang University of Technology,Liaoyang 111003,China;Key Laboratory for Chemical Drug Research of Shandong Province,Instiitute of Phamaceutical Sciences of Shandong Province,Jinan 250101,China)
出处
《合成化学》
CAS
北大核心
2020年第4期346-359,共14页
Chinese Journal of Synthetic Chemistry
基金
辽宁省自然科学基金资助项目(20180550016)
辽宁省教育厅科学研究项目(L2015383)
沈阳市科技计划项目(18-004-4-32)。
关键词
静脉血栓
抗凝血药物
合成
构效关系
靶点
抑制剂
机制
venous thrombosis
anticoagulant drug
synthesis
structure-activity relationship
target
inhibitor
mechanism
