Substituted 3-oxo-1,2,5-Thiadiazolidine 1,1-Dioxides: A New Class of Potential Mechanism-Based Inhibitors of Human Leukocyte Elastase and Cathepsin G

A series of substituted 3-oxo-1,2,5-thiadiazolidine 1,1-dioxides has been synthesized and their in vitro inhibitory activity toward human leukocyte elastase and cathepsin G was investigated. These compounds were found to inactivate the two enzymes efficiently and in a time-dependent fashion.

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Bibliographische Detailangaben
Veröffentlicht in:	Biochemical and biophysical research communications 1994-01, Vol.198 (1), p.341-349
Hauptverfasser:	Groutas, W.C., Kuang, R.Z., Venkataraman, R.
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Cathepsin G Cathepsins - antagonists & inhibitors Cathepsins - blood Cyclic S-Oxides - chemical synthesis Cyclic S-Oxides - pharmacology Humans Kinetics Leukocyte Elastase Leukocytes - enzymology Medical sciences Molecular Structure Pancreatic Elastase - antagonists & inhibitors Pancreatic Elastase - blood Pharmacology. Drug treatments Serine Endopeptidases Structure-Activity Relationship Thiadiazoles - chemical synthesis Thiadiazoles - pharmacology Time Factors
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Beschreibung
Zusammenfassung:	A series of substituted 3-oxo-1,2,5-thiadiazolidine 1,1-dioxides has been synthesized and their in vitro inhibitory activity toward human leukocyte elastase and cathepsin G was investigated. These compounds were found to inactivate the two enzymes efficiently and in a time-dependent fashion.
ISSN:	0006-291X 1090-2104
DOI:	10.1006/bbrc.1994.1048