Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Regular Articles
Novel Cephalosporins Synthesized by Amination of 2,5-Dihydroxybenzoic Acid Derivatives Using Fungal Laccases II
Annett Mikolasch, Timo Horst Johannes Niedermeyer, Michael Lalk, Sabine Witt, Simone Seefeldt, Elke Hammer, Frieder Schauer, Manuela Gesell Salazar, Susanne Hessel, Wolf-Dieter Jülich, Ulrike Lindequist
Author information
Keywords: cephalosporin, laccase, carbacephem, biotransformation, resistance
JOURNAL FREE ACCESS

2007 Volume 55 Issue 3 Pages 412-416

Details
Download PDF (99K)
Download citation RIS

(compatible with EndNote, Reference Manager, ProCite, RefWorks)

BIB TEX

(compatible with BibDesk, LaTeX)

Text
How to download citation
Contact us
Abstract

Sixteen novel cephalosporins were synthesized by amination of 2,5-dihydroxybenzoic acid derivatives with the aminocephalosporins cefadroxil, cefalexin, cefaclor, and the structurally related carbacephem loracarbef using laccases from Trametes sp. or Myceliophthora thermophila. All products inhibited the growth of several Gram positive bacterial strains in the agar diffusion assay, among them methicillin-resistant Staphylococcus aureus and vancomycin-resistant enterococci. The products protected mice against an infection with Staphylococcus aureus lethal to the control animals. Cytotoxicity and acute toxicity of the new compounds were negligible. The results show the usefulness of laccase for the synthesis of potential new antibiotics. The biological activity of the new compounds stimulates intensified pharmacological tests.

Content from these authors
© 2007 The Pharmaceutical Society of Japan
Previous article Next article
Favorites & Alerts

Recently viewed articles
Share this page
feedback
 Top