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Bioorg Med Chem. 2005 Apr 15;13(8):2847-58.

Synthesis and biological evaluation of penam sulfones as inhibitors of beta-lactamases.

Author information

1
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Kuwait University, PO Box 24923, Safat 13110, Kuwait. dphillips@hsc.edu.kw

Erratum in

  • Bioorg Med Chem. 2005 Nov 15;13(22):6276.

Abstract

The chemical synthesis of a series of new penam sulfone derivatives bearing a 2beta-substituted-oxyimino and -hydrazone substituents, their beta-lactamase inhibitory properties against selected enzymes representing class A and C beta-lactamases are reported. The oxime containing penam sulfones strongly inhibited the Escherichia coli TEM-1 and Klebsiella pneumoniae cefotaximase (CTX-1) enzymes, but moderately inhibited the Pseudomonas aeruginosa 46012 cephalosporinase; while the 2beta-substituted-hydrazone derivatives were generally less active against these enzymes. Furthermore, most of the inhibitors enhanced the antibacterial activities of piperacillin (PIP) and ceftazidime (CAZ) particularly against TEM-1 and CTX-1 producing bacterial strains.

PMID:
15781395
DOI:
10.1016/j.bmc.2005.02.020
[Indexed for MEDLINE]

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