Derivatives of 3-alkyl-N-hydroxysuccinimide: probing the effect of structure on bioactivity toward human leukocyte elastase
Groutas, William C. Brubaker, Michael J. Chong, Lee S. Epp, Jeffrey B. Huang, He Keller, C. E. McClenahan, Jerry J. Givens, R. S. Singh, R. Zandler, Melvin E.
Groutas, William C.
Brubaker, Michael J.
Chong, Lee S.
Epp, Jeffrey B.
Huang, He
Keller, C. E.
McClenahan, Jerry J.
Givens, R. S.
Singh, R.
Zandler, Melvin E.
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Time Period
Advisors
Original Date
Digitization Date
Issue Date
1994-02-01
Type
Article
Genre
Keywords
Research Support, U.S. Gov't, P.H.S.
Subjects (LCSH)
Leukocyte Elastase/chemistry
Pancreatic Elastase/chemistry
Succinimides/pharmacology
Pancreatic Elastase/chemistry
Succinimides/pharmacology
Citation
Drug design and discovery. 1994 Feb; 11(2): 149-57.
Abstract
A structure-activity relationship study was conducted in order to probe the nature of the interaction between some 3-alkyl-N-hydroxysuccinimide derivatives and human leukocyte elastase. The structural features in substituent X (structure I) that lead to the manifestation and optimization of inhibitory activity have been examined. The data suggest that the presence of an alkyl or aryl(sulfonyloxy) group in the active compounds may serve a triple purpose, namely, it functions as a good leaving group as dictated by the established mechanism of action of this class of compounds, secondly, it may enhance binding by assuming a favorable spatial orientation and, thirdly, it may increase the chemical reactivity of the carbonyl carbon in the bioactive compounds.
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Description
Full text of this article is not available in SOAR.
Publisher
Harwood Academic Publishers
Journal
Book Title
Series
Drug design and discovery
Drug Des Discov
Drug Des Discov
Digital Collection
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NLM
PubMed ID
DOI
ISSN
1055-9612
1026-7921
1026-7921