A 2-Aminobenzimidazole That Inhibits and Disperses Gram-Positive Biofilms through a Zinc-Dependent Mechanism

A 2-Aminobenzimidazole That Inhibits and Disperses Gram-Positive Biofilms through a Zinc-Dependent Mechanism

A number of 2-aminobenzimidazole derivatives were synthesized and screened for their ability to inhibit and disperse bacterial biofilms. From these compounds, a lead 2-aminobenzimidazole was identified that both inhibited and dispersed MRSA, vancomycin-resistant Enterococcus faecium, and Staphylococ...

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Veröffentlicht in:Journal of the American Chemical Society 2009-07, Vol.131 (29), p.9868-9869
Hauptverfasser: Rogers, Steven A, Huigens III, Robert W, Melander, Christian
Format: Artikel
Sprache:eng
Schlagworte:
Benzimidazoles - chemical synthesis
Benzimidazoles - chemistry
Benzimidazoles - pharmacology
Biofilms - drug effects
Biofilms - growth & development
Dose-Response Relationship, Drug
Gram-Positive Bacteria - drug effects
Magnetic Resonance Spectroscopy
Molecular Structure
Structure-Activity Relationship
Zinc - chemistry
Zinc - pharmacology
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Zusammenfassung:A number of 2-aminobenzimidazole derivatives were synthesized and screened for their ability to inhibit and disperse bacterial biofilms. From these compounds, a lead 2-aminobenzimidazole was identified that both inhibited and dispersed MRSA, vancomycin-resistant Enterococcus faecium, and Staphylococcus epidermidis biofilms. Mechanistic studies showed that the activity is Zn(II)-dependent, potentially via a direct zinc-chelating mechanism.
ISSN:0002-7863
1520-5126
DOI:10.1021/ja9024676