Progress of thrombus formation and research on the structure-activity relationship for antithrombotic drugs

Many populations suffer from thrombotic disorders such as stroke, myocardial infarction, unstable angina and thromboembolic disease. Thrombus is one of the major threatening factors to human health and the prevalence of cardio-cerebrovascular diseases induced by thrombus is growing worldwide, even some persons got rare and severe blood clots after receiving the AstraZeneca COVID vaccine unexpectedly. In terms of mechanism of thrombosis, antithrombotic drugs have been divided into three categories including anticoagulants, platelet inhibitors and fibrinolytics. Nowadays, a large number of new compounds possessing antithrombotic activities are emerging in an effort to remove the inevitable drawbacks of previously approved drugs such as the high risk of bleeding, a slow onset of action and a narrow therapeutic window. In this review, we describe the causes and mechanisms of thrombus formation firstly, and then summarize these reported active compounds as potential antithrombotic candidates based on their respective mechanism, hoping to promote the development of more effective bioactive molecules for treating thrombotic disorders. [Display omitted] •This review summarized the progress and mechanism of thrombus formation, and expounded three categories of approved antithrombotic agents.•A preliminary discussion about the structure-activity relationship (SAR) of synthetic antithrombotic molecules was also summarized.•This review provided evidence to design potent and selective thrombus inhibitors for target specific therapy to facilitate the further research.