The Gabriel-Colman rearrangement in biological systems: design, synthesis and biological evaluation of phthalimide and saccharin derivatives as potential mechanism-based inhibitors of human leukocyte elastase, cathepsin G and proteinase 3

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Issue Date
1995-02-01
Authors
Groutas, William C.
Chong, Lee S.
Venkataraman, Radhika
Epp, Jeffrey B.
Kuang, Rongze
Houser-Archield, Nadene
Hoidal, John R.
Advisor
Citation

Bioorganic & medicinal chemistry. 1995 Feb; 3(2): 187-93.

Abstract

The results of a structure-activity relationship study focusing on the interaction of a series of phthalimide and saccharin derivatives with leukocyte elastase, cathepsin G and proteinase 3 are described. The phthalimide derivatives were found to be inactive while some of the saccharin derivatives were found to be fair inhibitors of these enzymes.

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