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Enantioselective inhibition of human leukocyte elastase

Groutas, William C.
Brubaker, Michael J.
Venkataraman, Radhika
Stanga, Michael A.
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Issue Date
1992-08-15
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Article
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Keywords
Comparative Study,Research Support, U.S. Gov't, P.H.S.
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Citation
Archives of biochemistry and biophysics. 1992 Aug 15; 297(1): 144-6.
Abstract
(RS)-Diethyl-2-benzyl-succinate was resolved using alpha-chymotrypsin. The two enantiomers were then elaborated to yield (S)-(+) and (R)-(-)-3-benzyl-N-[(methyl-sulfonyl)oxy]succinimide and the inhibitory activity of the two enantiomers toward human leukocyte elastase was subsequently determined. The k2/KI values for the R and S isomers were found to be 330 and 1500 M-1 s-1, respectively.
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Publisher
Elsevier
Journal
Archives of Biochemistry and Biophysics
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DOI
ISSN
0003-9861
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