Journal
CHEMICAL & PHARMACEUTICAL BULLETIN
Volume 56, Issue 7, Pages 902-907Publisher
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.56.902
Keywords
laccase; catechol; biotransformation; beta-lactam antibiotic; resistance
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Novel cephalosporins, penicillins, and carbacephems were synthesized by amination of catechols with amino-beta-lactams like cefadroxil, amoxicillin, ampicillin and the structurally related carbacephem loracarbef using laccase from Trametes sp. All isolated monoaminated products inhibited the growth of several Gram positive bacterial strains in the agar diffusion assay, among them methicillin-resistant Staphylococcus aureus strains and vancomycin-resistant Enterococci. Observed differences in the cytotoxicity and in vivo activity in a Staphy-lococcus-infected, immune suppressed mouse model are discussed.
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