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Succinimide and saccharin-based enzyme-activated inhibitors of serine proteases
D C Martyn1, M J Moore, A D Abell
1Department of Chemistry, University of Canterbury, Christchurch, New Zealand.
Current Pharmaceutical Design
|July 3, 1999
Abstract:
The inhibition of human leukocyte elastase (HLE), and other serine proteases, by succinimide and saccharin-based compounds is reviewed. The succinimide compounds are unique in that the inactivating species is generated within the enzyme active site via a molecular rearrangement. The related saccharin derivatives also inactivate serine proteases by an enzyme-activated mechanism. Those factors effecting the potency, selectivity and stability of these important classes of inhibitor are discussed.