Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antibiotics, Antineoplastic / pharmacology
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Bacteria / drug effects
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Basidiomycota / metabolism*
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Cell Line, Tumor
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Chemical Phenomena
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Chemistry, Physical
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Chromatography, High Pressure Liquid
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Female
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Indicators and Reagents
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Laccase / metabolism*
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Magnetic Resonance Spectroscopy
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Mass Spectrometry
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Mice
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Mice, Inbred BALB C
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Microbial Sensitivity Tests
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Penicillins / biosynthesis*
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Penicillins / pharmacology
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Staphylococcal Infections / drug therapy
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Staphylococcal Infections / microbiology
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beta-Lactamase Inhibitors
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beta-Lactamases / metabolism
Substances
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Antibiotics, Antineoplastic
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Indicators and Reagents
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Penicillins
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beta-Lactamase Inhibitors
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Laccase
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beta-Lactamases