48 research outputs found
Preparation of Saccharin Derivatives of Amino Acids as Potential Peptidomimetic Building Blocks
2,4,5-Triphenylisothiazol-3(2H)-one 1,1-dioxides as inhibitors of human leukocyte elastase.
A series of substituted 2,4,5-triphenylisothiazol-3(2H)-one 1,1-dioxides 9 was synthesized and investigated as inhibitors of human leukocyte elastase (HLE). All compounds were found to inhibit HLE in a time-dependent manner and most of them exhibited kobs/[I] values > 300 Mâ 1sâ 1. The most potent 3-oxosultam of this series was 9l (kobs/[I] = 2440 Mâ 1sâ 1). Kinetic investigations performed with 9g and different substrate concentrations did not allow to clearly distinguish between a competitive or noncompetitive mode of inhibition. A more complex interaction is supported by the failure of a linear dependency of kobs values on the inhibitor concentration.Michael GĂźtschow, Markus Pietsch, Andrea Themann, Janine Fahrigâand Bärbel Schulzeâhttp://informahealthcare.com/doi/abs/10.1080/14756360500148783?journalCode=en