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.
Groutas
W C
WC
Department of Chemistry, Wichita State University, KS 67260.
Kuang
R
R
Venkataraman
R
R
D056649:Cathepsin G; D002403:Cathepsins / Q000037:antagonists & inhibitors* / Q000097:blood; D003499:Cyclic S-Oxides / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D007700:Kinetics; D019272:Leukocyte Elastase; D007962:Leukocytes / Q000201:enzymology*; D015394:Molecular Structure; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors* / Q000097:blood; D012697:Serine Endopeptidases; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D013997:Time Factors
D003499:Cyclic S-Oxides; D013830:Thiadiazoles; D002403:Cathepsins; D012697:Serine Endopeptidases; C534094:CTSG protein, human; D056649:Cathepsin G; D010196:Pancreatic Elastase; D019272:Leukocyte Elastase