TABLE 6

1,2,5-thiadiazolidin-3-one 1,dioxide derivatives blocking human PR3 activity

Embedded Imagekobs/[I]
PR3Elastase
M−1s−1
R1R2L
Isobutyl(m-COOCH3)BzlSO2Ph708063,600
Isobutyl(m-COCH)BzlSO2Ph10,30038,700
IsobutylBenzylSO2(p-Cl phenyl)16,200219,000
IsobutylBenzylSO2CH2(p-Cl phenyl)20,300165,000
  • Values are from Groutas et al. (1998).