Substituted 2-pyrones, 2-pyridones, and other congeners of elasnin as potential agents for the treatment of chronic obstructive lung diseases.
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.
D004549:Elastin / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D007962:Leukocytes / Q000201:enzymology; D008173:Lung Diseases, Obstructive / Q000188:drug therapy*; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors*; D011728:Pyridones / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D011728:Pyridones; D004549:Elastin; D010196:Pancreatic Elastase