Using N, N-dialkylated benzamidines as the novel P4 motifs, we have designed and
synthesized a class of 1-(2-naphthyl)-1H-pyrazole-5-carboxylamides as highly potent and …

The serine protease factor Xa is a critical enzyme in the blood coagulation cascade.
Recently, the inhibition of factor Xa has begun to emerge as an attractive strategy for the …

Venous and arterial thromboembolism are a major cause for morbidity and mortality. The list
of established drugs for the prevention of thrombus formation and embolisation includes …

Objective—In this study we test the hypothesis that blood/plasma-based prothrombinase
assays, rather than inhibition of purified factor Xa (fXa), are predictive of in vivo …

Factor Xa (fXa) is a crucial player in various thromboembolic disorders. Inhibition of fXa can
provide safe and effective antithrombotic effects. In this study, a series of anthranilamide …

Selective inhibitors of specific coagulation factors represent a new class of antithrombotic
agents, designed to overcome the limitations of traditional anticoagulants. Available clinical …

In an effort to identify a potential back-up to apixaban (Eliquis®), we explored a series of
diversified P4 moieties. Several analogs with substituted gem-dimethyl moieties replacing …

Although currently available anticoagulants are effective for the prevention and treatment of
thromboembolic disorders, they have several drawbacks. Low molecular weight heparin and …

Factor Xa (fXa) plays a critical role in the coagulation cascade, serving as the point of
convergence of the intrinsic and extrinsic pathways. Together with nonenzymatic cofactor Va …

Dear Sir, Once associated with the thrombus, blood coagulation factor Xa (FXa) still retains
its enzymatic activity, leading to the generation of thrombin and fibrin (1–3). The persistence …