Abstract
We report the synthesis and evaluation of 5-halogenated-1,2,3-triazoles as inhibitors of biotin protein ligase from Staphylococcus aureus. The halogenated compounds exhibit significantly improved antibacterial activity over their nonhalogenated counterparts. Importantly, the 5-fluoro-1,2,3-triazole compound 4c displays antibacterial activity against S. aureus ATCC49775 with a minimum inhibitory concentration (MIC) of 8 μg/mL.
Keywords:
Staphylococcus aureus; antibiotic; biotin protein ligase; enzyme inhibitor.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology*
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Binding Sites
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Biotin / metabolism
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Dose-Response Relationship, Drug
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Halogenation
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Humans
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Ligases / antagonists & inhibitors*
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Microbial Sensitivity Tests
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Models, Molecular
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Molecular Conformation
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Molecular Structure
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Protein Binding
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Staphylococcus aureus / drug effects*
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Staphylococcus aureus / enzymology*
Substances
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Anti-Bacterial Agents
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Enzyme Inhibitors
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Biotin
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Ligases