Design, synthesis, and in vitro inhibitory activity toward human leukocyte elastase, cathepsin G, and proteinase 3 of saccharin-derived sulfones and congeners
Groutas, William C. Epp, Jeffrey B. Venkataraman, Radhika Kuang, Rongze Truong, Tien M. McClenahan, Jerry J. Prakash, Om
Groutas, William C.
Epp, Jeffrey B.
Venkataraman, Radhika
Kuang, Rongze
Truong, Tien M.
McClenahan, Jerry J.
Prakash, Om
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1996-09-01
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Article
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Research Support, Non-U.S. Gov't,Research Support, U.S. Gov't, P.H.S.
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Citation
Bioorganic & medicinal chemistry. 1996 Sep; 4(9): 1393-400.
Abstract
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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Elsevier
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Bioorganic & medicinal chemistry
Bioorg. Med. Chem.
Bioorg. Med. Chem.
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0968-0896