Use of the 1,2,5-thiadiazolidin-3-one 1,1 dioxide and isothiazolidin-3-one 1,1 dioxide scaffolds in the design of potent inhibitors of serine proteinases.
The attachment of a phosphate leaving group to the 1,2,5-thiadiazolidin-3-one 1,1 dioxide and isothiazolidin-3-one 1,1 dioxide scaffolds was found to yield highly potent, time-dependent inhibitors of human leukocyte elastase (HLE).
Kuang
R
R
Department of Chemistry, Wichita State University, KS 67260, USA.
Venkataraman
R
R
Ruan
S
S
Groutas
W C
WC
D001665:Binding Sites; D015195:Drug Design; D006801:Humans; D007700:Kinetics; D019272:Leukocyte Elastase / Q000037:antagonists & inhibitors / Q000737:chemistry; D008958:Models, Molecular; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D013830:Thiadiazoles / Q000737:chemistry*
D015842:Serine Proteinase Inhibitors; D013830:Thiadiazoles; D019272:Leukocyte Elastase