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Design, synthesis, and in vitro inhibitory activity toward human leukocyte elastase, cathepsin G, and proteinase 3 of saccharin-derived sulfones and congeners

✍ Scribed by William C. Groutas; Jeffrey B. Epp; Radhika Venkataraman; Rongze Kuang; Tien My Truong; Jerry J. McClenahan; Om Prakash

Publisher: Elsevier Science
Year: 1996
Tongue: English
Weight: 604 KB
Volume: 4
Category: Article
ISSN: 0968-0896
DOI: 10.1016/0968-0896(96)00133-2

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✦ Synopsis

The inhibitory activity toward human leukocyte elastase (HLE), cathepsin G (Cat G), and proteinase 3 (PR 3) of a series of saccharin derivatives having a sulfinate leaving group was investigated. The results of this study revealed that (a) inhibitory activity is dependent on the nature and pKa of the leaving group, and (b) the synthesized saccharin derivatives exhibit selective inhibition toward HLE and PR 3, with low or no activity toward cathepsin G. The results of exploratory biochemical, HPLC and high-field 13C NMR studies are also described.

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