title: The inhibition of metallo-beta-lactamase by thioxo-cephalosporin derivatives.
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.
authors.affiliation: Department of Chemical and Biological Sciences, University of Huddersfield, Queensgate, Huddersfield HD1 3DH, UK.
authors.forename: Wing Y
authors.initials: WY
authors.lastname: Tsang
authors.forename: Anupma
authors.initials: A
authors.lastname: Dhanda
authors.forename: Christopher J
authors.initials: CJ
authors.lastname: Schofield
authors.forename: Jean-Marie
authors.initials: JM
authors.lastname: Frère
authors.forename: Moreno
authors.initials: M
authors.lastname: Galleni
authors.forename: Michael I
authors.initials: MI
authors.lastname: Page
mesh_terms: D001409:Bacillus cereus / Q000187:drug effects / Q000201:enzymology; D002511:Cephalosporins / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D065093:beta-Lactamase Inhibitors; D001618:beta-Lactamases / Q000378:metabolism
chemical_list: D002511:Cephalosporins; D004791:Enzyme Inhibitors; D065093:beta-Lactamase Inhibitors; D001618:beta-Lactamases