Design, synthesis, and in vitro inhibitory activity toward human leukocyte elastase, cathepsin G, and proteinase 3 of saccharin-derived sulfones and congeners
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Authors
Groutas, William C.
Epp, Jeffrey B.
Venkataraman, Radhika
Kuang, Rongze
Truong, Tien M.
McClenahan, Jerry J.
Prakash, Om
Advisors
Issue Date
1996-09-01
Type
Article
Keywords
Research Support, Non-U.S. Gov't , Research Support, U.S. Gov't, P.H.S.
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.
Table of Contents
Description
Full text of this article is not available in SOAR.
Publisher
Elsevier
Journal
Book Title
Series
Bioorganic & medicinal chemistry
Bioorg. Med. Chem.
Bioorg. Med. Chem.
PubMed ID
DOI
ISSN
0968-0896