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

Wing Y. Tsang, Anupma Dhanda, Christopher J. Schofield, Jean Marie Frère, Moreno Galleni, Michael I. Page

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24 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)1737-1739
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume14
Issue number7
DOIs
Publication statusPublished - Apr 2004

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  • Cite this

    Tsang, W. Y., Dhanda, A., Schofield, C. J., Frère, J. M., Galleni, M., & Page, M. I. (2004). The inhibition of metallo-β-lactamase by thioxo-cephalosporin derivatives. Bioorganic and Medicinal Chemistry Letters, 14(7), 1737-1739. https://doi.org/10.1016/j.bmcl.2004.01.047