Synthesis and evaluation of selected benzimidazole derivatives as potential antimicrobial agents
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Abstract© 2015 by the authors. A library of 53 benzimidazole derivatives, with substituents at positions 1, 2 and 5, were synthesized and screened against a series of reference strains of bacteria and fungi of medical relevance. The SAR analyses of the most promising results showed that the antimicrobial activity of the compounds depended on the substituents attached to the bicyclic heterocycle. In particular, some compounds displayed antibacterial activity against two methicillin-resistant Staphylococcus aureus (MRSA) strains with minimum inhibitory concentrations (MICs) comparable to the widely-used drug ciprofloxacin. The compounds have some common features; three possess 5-halo substituents; two are derivatives of (S)-2-ethanaminebenzimidazole; and the others are derivatives of one 2-(chloromethyl)-1Hbenzo[ d]imidazole and (1H-benzo[d]imidazol-2-yl)methanethiol. The results from the antifungal screening were also very interesting: 23 compounds exhibited potent fungicidal activity against the selected fungal strains. They displayed equivalent or greater potency in their MIC values than amphotericin B. The 5-halobenzimidazole derivatives could be considered promising broad-spectrum antimicrobial candidates that deserve further study for potential therapeutic applications.
CitationAlasmary, F.A.S., Snelling, A.M., Zain, M.E., Alafeefy, A.M., Awaad, A.S., Karodia, N. (2015) Synthesis and Evaluation of Selected Benzimidazole Derivatives as Potential Antimicrobial Agents. Molecules, 20(8), pp. 5206-15223.
PubMed ID26307956 (pubmed)
Description© 2015 The Authors. Published by MDPI. This is an open access article available under a Creative Commons licence. The published version can be accessed at the following link on the publisher’s website: https://doi.org/10.3390/molecules200815206
Except where otherwise noted, this item's license is described as Licence for published version: Creative Commons Attribution 4.0 International
- Synthesis and Evaluation of Selected Benzimidazole Derivatives as Potential Antimicrobial Agents.
- Authors: Alasmary FA, Snelling AM, Zain ME, Alafeefy AM, Awaad AS, Karodia N
- Issue date: 2015 Aug 20
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