Abstract
Several congeners of elasnin (I) have been synthesized and shown to inhibit human leukocyte elastase (HLE). The C-3 alkyl substituted 2-pyrones 11 and 12 were found to be the most effective inhibitors of the enzyme. These compounds are highly specific in their inhibitory activity.
Publication types
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Comparative Study
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Elastin / pharmacology
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Humans
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In Vitro Techniques
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Leukocytes / enzymology
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Lung Diseases, Obstructive / drug therapy*
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Pancreatic Elastase / antagonists & inhibitors*
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Pyridones / chemical synthesis
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Pyridones / pharmacology*
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Structure-Activity Relationship
Substances
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Pyridones
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Elastin
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Pancreatic Elastase