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FACTOR XA INHIBITORS

2006
The importance of factor Xa in the initiation and propagation of coagulation, as well as its pluripotential cellular properties, has been discussed previously. Considered collectively, the effects exhibited by this particular protease make it an attractive target for pharmacologic inhibition. Factor Xa inhibition can be classified and subcategorized as
ZHU BING-YAN   +5 more
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Anthranilamide inhibitors of factor Xa

Bioorganic & Medicinal Chemistry Letters, 2007
SAR about the B-ring of a series of N(2)-aroyl anthranilamide factor Xa (fXa) inhibitors is described. B-ring o-aminoalkylether and B-ring p-amine probes of the S1' and S4 sites, respectively, afforded picomolar fXa inhibitors that performed well in in vitro anticoagulation assays.
David, Mendel   +20 more
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Factor Xa inhibitors

2023
This chapter describes factor Xa as a key enzyme involved in thrombosis and clot formation. It considers factor Xa inhibitors as potential anticoagulants for the treatment of deep-vein thrombosis and pulmonary embolism. It also highlights the first factor Xa inhibitors to reach the market and covers the design process that led to the discovery of ...
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Inhibitors of Factor Xa

1999
Thrombin occupies a central position in thrombus formation and recently has been a target for the development of anticoagulant agents. As is well known, blood coagulation operates as a cascade or multiple enzymatic amplification process. In the classical intrinsic pathway, factor (f) IXa in the presence of fVIIIa, Ca2+ and phospholipid converts fX to ...
S. Kunitada, T. Nagahara, T. Hara
openaire   +3 more sources

Factor Xa Inhibitors

Current Pharmaceutical Design, 1996
Thrombin occupies a central position in thrombus formation and eventually has been a target to develop anticoagulant agents. Although both heparin and warfarin have been used as anticoagulants, a more useful, ideal anticoagulant is desired at bedside.
Satoshi Kunitada, Takayasu Nagahara
openaire   +1 more source

Heterogeneity of Synthetic Factor Xa Inhibitors

Current Pharmaceutical Design, 2005
Heparins and vitamin K antagonists are the landmarks of antithrombotic treatment. Both of them were discovered by serendipity; they are multi-targeted drugs and share several limitations. New molecules have been designed in order to be both more selective concerning their biological target and more homogeneous in their biochemical structure aiming at ...
Grigoris T, Gerotziafas, Meyer M, Samama
openaire   +2 more sources

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