Abstract
3,4,5-Trisubstituted isoxazolines (2) and isoxazoles (3) were prepared and evaluated for their in vitro and in vivo antithrombotic efficacy. They were compared to 3,5,5-trisubstituted isoxazolines (1) for Factor Xa selectivity and potency. They were also compared in an arterio-venous (A-V) shunt model of thrombosis.
MeSH terms
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Animals
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Crystallography, X-Ray
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Factor Xa Inhibitors*
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Isoxazoles / chemistry
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Isoxazoles / pharmacokinetics
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Isoxazoles / pharmacology*
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Models, Molecular
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Rabbits
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Serine Proteinase Inhibitors / chemistry
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Serine Proteinase Inhibitors / pharmacokinetics
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Serine Proteinase Inhibitors / pharmacology*
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Structure-Activity Relationship
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Thrombosis / prevention & control
Substances
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Factor Xa Inhibitors
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Isoxazoles
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Serine Proteinase Inhibitors