The inhibition of metallo-beta-lactamase by thioxo-cephalosporin derivatives |
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Authors: | Tsang Wing Y Dhanda Anupma Schofield Christopher J Frère Jean-Marie Galleni Moreno Page Michael I |
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Affiliation: | Department of Chemical and Biological Sciences, University of Huddersfield, Queensgate, Huddersfield HD1 3DH, UK. |
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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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