The discovery and subsequent clinical use of coumarins, in the 1950s and of heparin in the
1970s allowed, for the first time, rational treatment of thrombotic diseases. However, in spite …

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 …

In recent years, the understanding of the causes and mechanisms of thromboembolic
disorders has rapidly grown. The established therapeutic strategies obviously have their …

Factor Xa (fXa) is a serine protease, which plays a pivotal role in the coagulation cascade.
To improve the oral anticoagulant activity of fXa inhibitors containing a 1, 4-diazepane …

The limitations of conventional anticoagulants have stimulated the development of new
anticoagulants. The central position of factor Xa (FXa) at the junction of the intrinsic and …

Publisher Summary In recent times, research on novel thrombin inhibitors, the exploration of
the applications of oral thrombin inhibitors and the development of therapeutically useful low …

Highly potent and selective substrate analogue factor Xa inhibitors were obtained by
incorporation of non-basic or modestly basic P1 residues known from the development of …

The direct oral anticoagulants targeting coagulation factor Xa or thrombin are widely used as
alternatives to vitamin K antagonists in the management of venous thromboembolism and …

A variety of P4 motifs have been examined to increase the binding affinity and in vitro
anticoagulant potency of our biphenyl 1-(2-naphthyl)-1H-pyrazole-5-carboxylamide-based …