Results 251 to 260 of about 655,147 (306)
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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
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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
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2023
Abstract Oral factor Xa (FXa) inhibitors exert their antithrombotic effects and increase the risk of bleeding by their effects on the coagulation system. The oral direct FXa inhibitors are highly potent, reversible active-site inhibitors of FXa with good bioavailability, rapid onset, and used in a daily standard dose without laboratory ...
Agneta Siegbahn +3 more
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Abstract Oral factor Xa (FXa) inhibitors exert their antithrombotic effects and increase the risk of bleeding by their effects on the coagulation system. The oral direct FXa inhibitors are highly potent, reversible active-site inhibitors of FXa with good bioavailability, rapid onset, and used in a daily standard dose without laboratory ...
Agneta Siegbahn +3 more
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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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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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Anthranilamide inhibitors of factor Xa
Bioorganic & Medicinal Chemistry Letters, 2007SAR 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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Mayo Clinic proceedings, 2019
OBJECTIVE To explore the efficacy and safety of direct oral factor Xa inhibitors in the treatment of cancer-associated acute venous thromboembolism (VTE).
H. Fuentes +6 more
semanticscholar +1 more source
OBJECTIVE To explore the efficacy and safety of direct oral factor Xa inhibitors in the treatment of cancer-associated acute venous thromboembolism (VTE).
H. Fuentes +6 more
semanticscholar +1 more source
Perspectives in Drug Discovery and Design, 1994
Factor Xa is the serine protease that activates prothrombin to yield thrombin. Inhibitors of factor Xa play a crucial role in curtailing thrombin generation. Two key factor Xa inhibitors that are found in blood are antithrombin III and tissue factor pathway inhibitor.
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Factor Xa is the serine protease that activates prothrombin to yield thrombin. Inhibitors of factor Xa play a crucial role in curtailing thrombin generation. Two key factor Xa inhibitors that are found in blood are antithrombin III and tissue factor pathway inhibitor.
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Rivaroxaban: An Oral Factor Xa Inhibitor
Clinical Therapeutics, 2013Currently available anticoagulants utilized for venous thromboembolism (VTE) treatment and prevention and stroke prevention in patients with atrial fibrillation (AF) have proven effectiveness but are not optimally utilized because of barriers such as the need for subcutaneous administration and requisite routine laboratory monitoring.
Tyan F, Thomas +2 more
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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
Richard C. Becker, Frederick A. Spencer
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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
Richard C. Becker, Frederick A. Spencer
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Heterogeneity of Synthetic Factor Xa Inhibitors
Current Pharmaceutical Design, 2005Heparins 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
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Phenyltriazolinones as potent factor Xa inhibitors
Bioorganic & Medicinal Chemistry Letters, 2010We have discovered that phenyltriazolinone is a novel and potent P1 moiety for coagulation factor Xa. X-ray structures of the inhibitors with a phenyltriazolinone in the P1 position revealed that the side chain of Asp189 has reoriented resulting in a novel S1 binding pocket which is larger in size to accommodate the phenyltriazolinone P1 substrate.
Mimi L, Quan +12 more
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