Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2004 Apr 5;14(7):1737-9.

The inhibition of metallo-beta-lactamase by thioxo-cephalosporin derivatives.

Author information

1
Department of Chemical and Biological Sciences, University of Huddersfield, Queensgate, Huddersfield HD1 3DH, UK.

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.

PMID:
15026061
DOI:
10.1016/j.bmcl.2004.01.047
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center