Abstract
A library of 5''-modified neomycin derivatives were synthesized for an antibacterial structure-activity optimization strategy. Two leads exhibited prominent activity against both methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE). Antibacterial activities were measured when combined with other clinically used antibiotics. Significant synergistic activities were observed, which may lead to the development of novel therapeutic practices in the battle against infectious bacteria.
Publication types
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Research Support, N.I.H., Extramural
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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Drug Synergism
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Drug Therapy, Combination
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Enterococcus / drug effects
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Gram-Negative Bacteria / drug effects*
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Gram-Positive Bacteria / drug effects*
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Humans
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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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Neomycin* / analogs & derivatives
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Neomycin* / chemical synthesis
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Neomycin* / chemistry
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Neomycin* / pharmacology
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Structure-Activity Relationship
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Vancomycin Resistance
Substances
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Anti-Bacterial Agents
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Neomycin