Abstract
The present work demonstrates that the 1,3-diazetidine-2,4-dione nucleus is effective as a scaffold of serine protease inhibitors. Compound 1 displayed high activity against human cathepsin G and alpha-chymotrypsin (0.39, 0.69 nM). Compound 6 exhibited 0.85 nM inhibition of human chymase. Compound 10 was a selective inhibitor against human neutrophil elastase.
MeSH terms
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Azetidines / chemistry
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Azetidines / pharmacology*
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Cathepsin G
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Cathepsins / antagonists & inhibitors*
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Chymotrypsin / antagonists & inhibitors*
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Humans
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Leukocyte Elastase / antagonists & inhibitors
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Serine Endopeptidases
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Serine Proteinase Inhibitors / chemistry
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Serine Proteinase Inhibitors / pharmacology*
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Substrate Specificity
Substances
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Azetidines
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Serine Proteinase Inhibitors
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Cathepsins
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Serine Endopeptidases
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Chymotrypsin
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alpha-chymotrypsin
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CTSG protein, human
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Cathepsin G
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Leukocyte Elastase