{Reference Type}: Journal Article
{Title}: Contemporary medicinal-chemistry strategies for discovery of blood coagulation factor Xa inhibitors.
{Author}: Hao X;Zuo X;Kang D;Zhang J;Song Y;Liu X;Zhan P;
{Journal}: Expert Opin Drug Discov
{Volume}: 14
{Issue}: 9
{Year}: 09 2019
{Factor}: 7.05
{DOI}: 10.1080/17460441.2019.1626821
{Abstract}: Introduction: Thrombosis is a common causal pathology for stroke, acute coronary syndrome and venous thromboembolism disorders, which are the leading cause of death worldwide. Anticoagulants have exhibited a crucial role in the prevention and treatment of thrombotic diseases. Factor Xa (FXa) is a serine protease with a central role in activating the complex blood coagulation cascade, and it is therefore regarded as an attractive target for antithrombotic agents. Areas covered: The authors review the current status of medicinal chemistry strategies for the discovery of novel FXa inhibitors and provide their expert perspectives on their future development. Expert opinion: Even if only a number of small-molecule FXa inhibitors have been reported to date, all currently available FXa inhibitors are associated with significant risk of bleeding, which may become life-threatening. There is, therefore, an urgent and unmet demand for potent novel FXa inhibitors that are potent treatments for thrombotic disorders, but which have a reduced risk of bleeding if their use is to be increasingly favored.