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The inhibition of metallo-beta-lactamase by thioxo-cephalosporin derivatives.

Abstract:
The 8-thioxocephalosporins are poor substrates for the B. cereus metallo beta-lactamase (k(cat)/K(m)=61.4M(-1) s(-1)) and act as weak competitive inhibitors (K(i) approximately 700 microM). The hydrolysis product of thioxocephalosporin, a thioacid, also inhibits the enzyme competitively with a K(i)=96 microM, whereas the cyclic thioxo-piperazinedione, formed by intramolecular aminolysis of thioxocephalexin has a K(i) of 29 microM.
Publication status:
Published

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Publisher copy:
10.1016/j.bmcl.2004.01.047

Authors


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Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Organic Chemistry
Role:
Author
Journal:
Bioorganic and medicinal chemistry letters More from this journal
Volume:
14
Issue:
7
Pages:
1737-1739
Publication date:
2004-04-01
DOI:
EISSN:
1464-3405
ISSN:
0960-894X
Language:
English
Keywords:
Pubs id:
pubs:38980
UUID:
uuid:fccd64c9-7b15-4f56-8690-2c26f6cbe33e
Local pid:
pubs:38980
Source identifiers:
38980
Deposit date:
2012-12-19

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