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

Research output: Contribution to journalArticlepeer-review

25 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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