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).