Abstract
1-Oxacephem derivatives were evaluated as a novel series of chymase inhibitors. The structure-activity relationship studies of 1-oxacephems led to compounds 15, which exhibited 27 nM inhibition of human chymase and improvement of stability in human plasma (t 1/2 1.5 h).
MeSH terms
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Cephalosporins / blood
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Cephalosporins / chemical synthesis*
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Cephalosporins / chemistry
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Cephalosporins / pharmacology
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Chymases
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Enzyme Stability
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Humans
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Models, Molecular
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Molecular Structure
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Plasma / chemistry
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Serine Endopeptidases / chemistry
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Serine Endopeptidases / metabolism*
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Serine Proteinase Inhibitors / blood
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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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Structure-Activity Relationship
Substances
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Cephalosporins
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Serine Proteinase Inhibitors
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Serine Endopeptidases
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Chymases