Synthesis and evaluation of selected benzimidazole derivatives as potential antimicrobial agents
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.Citation
Alasmary, 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.Publisher
MDPIJournal
MoleculesPubMed ID
26307956 (pubmed)Additional Links
https://www.mdpi.com/1420-3049/20/8/15206Type
Journal articleLanguage
enDescription
© 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/molecules200815206ISSN
1420-3049EISSN
1420-3049ae974a485f413a2113503eed53cd6c53
10.3390/molecules200815206
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Except where otherwise noted, this item's license is described as Licence for published version: Creative Commons Attribution 4.0 International
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