Abstract
We designed a few polymyxin derivatives which exhibit broad-spectrum antimicrobial activity. Lead compound P1 could disrupt bacterial membranes rapidly without developing resistance, inhibit biofilms formed by E. coli, and exhibit excellent in vivo activity in an MRSA-infected thigh burden mouse model.
MeSH terms
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Anti-Bacterial Agents / chemical synthesis
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology*
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Biofilms / drug effects
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Dose-Response Relationship, Drug
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Escherichia coli / drug effects*
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Methicillin-Resistant Staphylococcus aureus / drug effects*
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Microbial Sensitivity Tests
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Molecular Conformation
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Polymyxins / chemical synthesis
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Polymyxins / chemistry
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Polymyxins / pharmacology*
Substances
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Anti-Bacterial Agents
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Polymyxins