Synthesis and Evaluation of Selected Benzimidazole Derivatives as Potential Antimicrobial AgentsReport as inadecuate




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Chemistry Department, College of Science, King Saud University, Riyadh 11362, Saudi Arabia

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Centre for Pharmaceutical Engineering Science, Faculty of Life Sciences, University of Bradford, Richmond Road, Bradford BD7 1DP, UK

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Botany and Microbiology Department, College of Science, King Saud University, Riyadh 11362, Saudi Arabia

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Department of Pharmaceutical Chemistry, College of Pharmacy, Sattam bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia

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Pharmacognosy Department, College of Pharmacy, Salman bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia

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Faculty of Science and Engineering, University of Wolverhampton, Wulfruna Street, Wolverhampton WV1 1LY, UK





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Authors to whom correspondence should be addressed.



Academic Editor: Derek J. McPhee

Abstract 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-1H-benzodimidazole and 1H-benzodimidazol-2-ylmethanethiol. 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. View Full-Text

Keywords: benzimidazole; heterocycle; antibacterial activity; antifungal activity; resistance; Gram-negative; Gram-positive benzimidazole; heterocycle; antibacterial activity; antifungal activity; resistance; Gram-negative; Gram-positive





Author: Fatmah A. S. Alasmary 1,2,* , Anna M. Snelling 2, Mohammed E. Zain 3, Ahmed M. Alafeefy 4, Amani S. Awaad 5 and Nazira Karodia 2,6,*

Source: http://mdpi.com/



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