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

[en] The 8-thioxocephalosporins are poor substrates for the B. cereus metallo beta-lactamase (k(cat)/K-m = 61.4 M-1 s(-1)) and act as weak competitive inhibitors (K-i similar to 700 muM). The hydrolysis product of thioxocephalosporin, a thioacid, also inhibits the enzyme competitively with a K-i = 96 muM, whereas the cyclic thioxo-piperazinedione, formed by intramolecular aminolysis of thioxo-cephalexin has a K-i of 29 muM. (C) 2004 Elsevier Ltd. All rights reserved.

Disciplines :

Pharmacy, pharmacology & toxicology
Chemistry

Author, co-author :

Tsang, W. Y.

Dhanda, A.

Schofield, C. J.

Frère, Jean-Marie ; Université de Liège - ULiège > Département des sciences de la vie > Département des sciences de la vie

Galleni, Moreno ; Université de Liège - ULiège > Département des sciences de la vie > Macromolécules biologiques

Page, M. I.

Language :

English

Title :

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

Publication date :

05 April 2004

Journal title :

Bioorganic and Medicinal Chemistry Letters

ISSN :

0960-894X

eISSN :

1464-3405

Publisher :

Pergamon-Elsevier Science Ltd, Oxford, United Kingdom

Volume :

Issue :

Pages :

1737-1739

Peer reviewed :

Peer Reviewed verified by ORBi

Available on ORBi :

since 23 November 2015

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