Cardiovascular and cerebrovascular disorders continue to be the leading cause of death globally. Arterial and venous thrombosis might lead to acute coronary syndrome (ACS), myocardial infarction (MI), stroke, venous thromboembolism (VTE), peripheral artery occlusion (PAO), deep vein thrombosis (DVT), or disseminated intravascular thrombosis (DIT). Multiple factors are involved in the development of intravascular thrombosis, while abnormalities in the thrombolytic mechanisms might also lead to the ineffective removal of thrombus and seem to be associated with these pathologies. Tissue plasminogen activators, platelet Glycoprotein GPIIb/IIIa antagonists, adenosine diphosphate (ADP) receptor antagonists, coumarins, and low molecular weight heparins are currently being used to prevent thrombosis; these drugs have however, some inherent problems and limitations. Many labs have therefore active projects to search next generation anti-thrombotic agents such as orally active direct thrombin inhibitors, tissue factor inhibitors, Factor Xa inhibitors, and anti-platelet agents from both synthetic and natural sources.