Abstract
We describe the structure-based design and synthesis of highly potent, orally bioavailable tissue factor/factor VIIa inhibitors which interfere with the coagulation cascade by selective inhibition of the extrinsic pathway.
MeSH terms
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Administration, Oral
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Animals
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Anticoagulants / chemical synthesis
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Anticoagulants / chemistry*
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Anticoagulants / pharmacology*
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Biological Availability
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Crystallography, X-Ray
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Drug Design
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Factor VIIa / antagonists & inhibitors*
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Glycine / analogs & derivatives
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Glycine / chemistry
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Humans
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Molecular Structure
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Rats
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Serine Proteinase Inhibitors / chemical synthesis
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Serine Proteinase Inhibitors / chemistry*
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Serine Proteinase Inhibitors / pharmacology*
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Thromboplastin / antagonists & inhibitors*
Substances
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Anticoagulants
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Serine Proteinase Inhibitors
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2-phenylglycine
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Thromboplastin
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Factor VIIa
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Glycine