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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

Chem Pharm Bull (Tokyo). 2007 Mar;55(3):412-6.

PMID: 17329882

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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP147103944 Cefadroxil Related Compound I Cefadroxil Related Compound I 147103-94-4 Price
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