Abstract
A new class of novel bis-benzimidazole diamidine compounds have been synthesized and evaluated for in vitro antibacterial activities, including drug-resistant bacterial strains. Anti-MRSA and anti-VRE activities of the most potent compound 1 were more active than Vancomycin. The mechanism of action for this class of compounds appears to be different from existing antibiotics. Bis-benzimidazole diamidine compounds have potential for further investigation as a new class of potent anti-MRSA and anti-VRE agents.
MeSH terms
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / classification
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Anti-Bacterial Agents / pharmacology
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Benzimidazoles / chemical synthesis*
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Benzimidazoles / classification
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Benzimidazoles / pharmacology*
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Drug Resistance, Multiple, Bacterial / drug effects
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Enterococcus faecium / drug effects*
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Methicillin Resistance / drug effects
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Methicillin-Resistant Staphylococcus aureus / drug effects*
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Structure-Activity Relationship
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Vancomycin Resistance / drug effects
Substances
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Anti-Bacterial Agents
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Benzimidazoles
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bis-benzimidazole