Specific inhibition of human leukocyte elastase by substituted alpha-pyrones

Summary Severala-pyrones have been synthesized and investigated for their in vitro inhibitory activity usinga-chymotrypsin (a-CT), porcine pancreatic elastase, (PPE) and human leukocyte elastase (HLE). 4-Hydroxy-6-undecyl-2H-pyran-2-one4, 4-Hydroxy-6-(1-butyl)heptyl]-2H-pyran-2-one5 and 4-Methoxy-6-(1-butyl)heptyl]-2H-pyran-2-one6 were found to be specific inhibitors of HLE. These compounds constitute a promising new class of HLE inhibitors.Acknowledgments. We are grateful to the Petroleum Research Fund of the American Chemical Society (Grant No. 13058-B4), the American Lung Association and the Office of Sponsored Research of Wichita State University for generous financial support of this work. This work was also supported by NHLBIGrant 5PO1HL20994 and the Council for Tobacco Research, USA-Inc. Grant 901B.