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

Tsang, Wing Y., Dhanda, Anupma, Schofield, Christopher J., Frere, Jean-Marie, Galleni, Moreno and Page, Michael I. (2004) The inhibition of metallo-β-lactamase by thioxo-cephalosporin derivatives. Bioorganic & Medicinal Chemistry Letters, 14 (7). pp. 1737-1739. ISSN 0960-894X

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The 8-thioxocephalosporins are poor substrates for the B. cereus metallo β-lactamase (kcat/Km=61.4 M−1 s−1) and act as weak competitive inhibitors (Ki 700 μM). The hydrolysis product of thioxocephalosporin, a thioacid, also inhibits the enzyme competitively with a Ki=96 μM, whereas the cyclic thioxo-piperazinedione, formed by intramolecular aminolysis of thioxocephalexin has a Ki of 29 μM.

Item Type: Article
Subjects: Q Science > Q Science (General)
Q Science > QD Chemistry
Schools: School of Applied Sciences
School of Applied Sciences > Biomolecular Sciences Research Centre
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Date Deposited: 08 Feb 2008 15:24
Last Modified: 07 Apr 2018 18:45


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