Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
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Novel Penicillins Synthesized by Biotransformation Using Laccase from Trametes spec.
Annett MikolaschTimo Horst Johannes NiedermeyerMichael LalkSabine WittSimone SeefeldtElke HammerFrieder SchauerManuela GesellSusanne HesselWolf-Dieter JülichUlrike Lindequist
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2006 Volume 54 Issue 5 Pages 632-638


Eight novel penicillins were synthesized by heteromolecular reaction of ampicillin or amoxicillin with 2,5-dihydroxybenzoic acid derivatives using a laccase from Trametes spec. 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 untreated animals. Cytotoxicity and acute toxicity of the new compounds were neglectable. 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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© 2006 The Pharmaceutical Society of Japan
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