新型小分子抗凝血药物的合成、作用机制及构效关系研究进展

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。

Synthesis,Action Mechanism and Structure-activity Relationship of Novel Small Molecule Anticoagulant Drugs

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.