Results 221 to 230 of about 242,673 (264)
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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 +1 more
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Sulfonamidolactam inhibitors of coagulation factor Xa
Bioorganic & Medicinal Chemistry Letters, 2008As part of an effort to identify novel backups for previously reported pyrazole-based coagulation Factor Xa inhibitors, the pyrazole 5-carboxamide moiety was replaced by 3-(sulfonylamino)-2-piperidone. This led to the identification of a structurally diverse chemotype that was further optimized to incorporate neutral or weakly basic aryl and heteroaryl
Suanne Nakajima +13 more
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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.
Steven Sheriff +12 more
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The direct factor Xa inhibitor rivaroxaban
Medical Journal of Australia, 2009Warfarin and heparin are the traditional mainstay anticoagulant therapies for treating thromboembolic disease. These drugs, with a documented history of utility, also have inherent difficulties in usage; in particular, the complicated monitoring and numerous drug-drug interactions of warfarin, and the need for parenteral administration of heparins. New
Timothy A. Brighton +2 more
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Factor Xa inactivation by a heparinized hydrogel
Thrombosis Research, 1986Incubating Factor Xa and plasma in the presence of "beads" of a heparinized hydrogel (heparin-PVA) resulted in a loss of Factor Xa activity as measured by clotting time or chromogenic substrate assays. This loss in activity was attributed to the activity of the heparin immobilized to the polyvinyl alcohol (PVA) hydrogel.
Gordon Rollason, Michael V. Sefton
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Synthetic inhibitors of coagulation factor Xa
Expert Opinion on Investigational Drugs, 1999The antithrombotic efficacy of low molecular weight heparins suggest that specific inhibition of blood coagulation factor Xa (fXa) is an appropriate target for drug discovery. Clinical evidence also supports the effectiveness of warfarin, an orally bioavailable non-specific anticoagulant.
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Isoxazolines and isoxazoles as factor Xa inhibitors
Bioorganic & Medicinal Chemistry Letters, 2000AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Ruth R. Wexler +7 more
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Factor Xa-A pleuripotential protease.
Journal of thrombosis and thrombolysis, 2003A current view of vascular thrombosis emphasizes the importance of cellular surface biochemistry and the integrated contribution of platelets, monocytes and endothelial cells that contribute to atherothrombosis. Initiation of coagulation occurs on tissue-factor bearing cells, while amplification (or priming) requires activation of platelets and ...
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Biochemistry, 1990
Factor Xa modified by reductive methylation (greater than 92%) loses the capacity to bind heparin as determined both by gel chromatography and by sedimentation equilibrium ultracentrifugation. The kinetic properties of methylated factor Xa differ, with respect to KM and Vmax for a synthetic tripeptide substrate and for antithrombin III inhibition rate ...
Whyte G. Owen, Barbara A.L. Owen
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Factor Xa modified by reductive methylation (greater than 92%) loses the capacity to bind heparin as determined both by gel chromatography and by sedimentation equilibrium ultracentrifugation. The kinetic properties of methylated factor Xa differ, with respect to KM and Vmax for a synthetic tripeptide substrate and for antithrombin III inhibition rate ...
Whyte G. Owen, Barbara A.L. Owen
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Biochemical and Biophysical Research Communications, 1993
A series of 3-amidinoaryl-2-[4-[ [(3S)-3-pyrrolidinyl]oxy]phenyl] propanoic acids have been investigated for development of a novel factor Xa inhibitor, possessing a potent inhibitory activity for factor Xa and a selectivity for factor Xa compared to thrombin. In order to study the structure-activity relationships and the selectivity, models of factors
S.-I. Katakura +3 more
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A series of 3-amidinoaryl-2-[4-[ [(3S)-3-pyrrolidinyl]oxy]phenyl] propanoic acids have been investigated for development of a novel factor Xa inhibitor, possessing a potent inhibitory activity for factor Xa and a selectivity for factor Xa compared to thrombin. In order to study the structure-activity relationships and the selectivity, models of factors
S.-I. Katakura +3 more
openaire +3 more sources