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  • Title: The inhibition of metallo-beta-lactamase by thioxo-cephalosporin derivatives.
    Author: Tsang WY, Dhanda A, Schofield CJ, Frère JM, Galleni M, Page MI.
    Journal: Bioorg Med Chem Lett; 2004 Apr 05; 14(7):1737-9. PubMed ID: 15026061.
    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.
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