Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
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Novel Cephalosporins Synthesized by Amination of 2,5-Dihydroxybenzoic Acid Derivatives Using Fungal Laccases II
Annett MikolaschTimo Horst Johannes NiedermeyerMichael LalkSabine WittSimone SeefeldtElke HammerFrieder SchauerManuela Gesell SalazarSusanne HesselWolf-Dieter JülichUlrike Lindequist
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2007 Volume 55 Issue 3 Pages 412-416


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.

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© 2007 The Pharmaceutical Society of Japan
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