Benzimidazole-based antibacterial agents against Francisella tularensis |
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Authors: | Kunal Kumar Divya Awasthi Seung-Yub Lee Jason E. Cummings Susan E. Knudson Richard A. Slayden Iwao Ojima |
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Affiliation: | 1. Department of Chemistry and Institute of Chemical Biology & Drug Discovery, Stony Brook University, Stony Brook, NY 11794-3400, United States;2. Department of Microbiology, Immunology and Pathology, Colorado State University, Fort Collins, CO 80523-0922, United States |
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Abstract: | Francisella tularensis is a highly virulent pathogenic bacterium. In order to identify novel potential antibacterial agents against F. tularensis, libraries of trisubstituted benzimidazoles were screened against F. tularensis LVS strain. In a preliminary screening assay, remarkably, 23 of 2,5,6- and 2,5,7-trisubstituted benzimidazoles showed excellent activity exhibiting greater than 90% growth inhibition at 1 μg/mL. Among those hits, 21 compounds showed MIC90 values in the range of 0.35–48.6 μg/mL after accurate MIC determination. In ex vivo efficacy assays, four of these compounds exhibited 2–3 log reduction in colony forming units (CFU) per mL at concentrations of 10 and 50 μg/mL. |
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Keywords: | Antibacterial Benzimidazole |
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