Abstract
We designed a class of small dimeric cyclic guanidine derivatives which display potent antibacterial activity against both multidrug-resistant Gram-negative and Gram-positive bacteria. They could compromise bacterial membranes without developing resistance, inhibit biofilms formed by E. coli, and exhibit excellent in vivo activity in the MRSA-infected thigh burden mouse model.
MeSH terms
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Animals
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Anti-Bacterial Agents / chemistry*
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Anti-Bacterial Agents / pharmacology*
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Anti-Bacterial Agents / therapeutic use
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Cyclization
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Dimerization
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Escherichia coli / drug effects*
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Escherichia coli Infections / drug therapy
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Guanidine / analogs & derivatives*
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Guanidine / pharmacology*
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Guanidine / therapeutic use
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Humans
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Methicillin-Resistant Staphylococcus aureus / drug effects*
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Mice
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Microbial Sensitivity Tests
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Staphylococcal Infections / drug therapy
Substances
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Anti-Bacterial Agents
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Guanidine