Abstract
A series of 22 novel 1,2-disubstituted-1H-benzimidazole-N-alkylated-5- carboxamidine derivatives were synthesized and evaluated for in vitro antibacterial activity against S. aureus and methicillin resistant S. aureus (MRSA), E. coli, E. faecalis and for antifungal activity against C. albicans. Compound 59 [1-(2,4-dichlorobenzyl)-N- (2-diethylaminoethyl)-1H-benzimidazole-5-carboxamidine], with a 3,4-dichlorophenyl group at the C-2 position, displayed the greatest activity (MIC = 3.12 microg/mL against both some bacteria and the fungus C. albicans).
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amidines / chemical synthesis*
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Amidines / chemistry
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Amidines / pharmacology*
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Anti-Bacterial Agents / chemical synthesis*
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Anti-Bacterial Agents / pharmacology*
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Antifungal Agents / chemical synthesis
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Antifungal Agents / chemistry
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Antifungal Agents / pharmacology*
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Benzimidazoles / chemistry*
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Candida albicans / drug effects
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Magnetic Resonance Spectroscopy
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Mass Spectrometry
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Methicillin Resistance*
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Microbial Sensitivity Tests
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Molecular Structure
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Staphylococcus aureus / drug effects
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Structure-Activity Relationship
Substances
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Amidines
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Anti-Bacterial Agents
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Antifungal Agents
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Benzimidazoles
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benzimidazole