Development of benzimidazole-based derivatives as antimicrobial agents and their synergistic effect with colistin against gram-negative bacteria
Gram-negative bacteria pose a distinctive risk worldwide, especially with the evolution of major resistance to carbapenems, fluoroquinolones and colistin. Therefore, development of new antibacterial agents to target Gram-negative infections is of utmost importance. Using phenotypic screening, we syn...
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| Hauptverfasser: | , , , , , , , , , , |
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| Dokumenttyp: | Article (Journal) |
| Sprache: | Englisch |
| Veröffentlicht: |
[15 January 2020]
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| In: |
European journal of medicinal chemistry
Year: 2019, Jahrgang: 186 |
| ISSN: | 1768-3254 |
| DOI: | 10.1016/j.ejmech.2019.111850 |
| Online-Zugang: | Verlag, lizenzpflichtig, Volltext: https://doi.org/10.1016/j.ejmech.2019.111850 Verlag, lizenzpflichtig, Volltext: http://www.sciencedirect.com/science/article/pii/S0223523419310025 
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| Verfasserangaben: | Eman M. E. Dokla, Nader S. Abutaleb, Sandra N. Milik, Daoyi Li, Karim El-Baz, Menna-Allah W. Shalaby, Rawan Al-Karaki, Maha Nasr, Christian D. Klein, Khaled A. M. Abouzid, Mohamed N. Seleem |
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| 245 | 1 | 0 | |a Development of benzimidazole-based derivatives as antimicrobial agents and their synergistic effect with colistin against gram-negative bacteria |c Eman M. E. Dokla, Nader S. Abutaleb, Sandra N. Milik, Daoyi Li, Karim El-Baz, Menna-Allah W. Shalaby, Rawan Al-Karaki, Maha Nasr, Christian D. Klein, Khaled A. M. Abouzid, Mohamed N. Seleem |
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| 520 | |a Gram-negative bacteria pose a distinctive risk worldwide, especially with the evolution of major resistance to carbapenems, fluoroquinolones and colistin. Therefore, development of new antibacterial agents to target Gram-negative infections is of utmost importance. Using phenotypic screening, we synthesized and tested thirty-one benzimidazole derivatives against E. coli JW55031 (TolC mutant strain). Compound 6c showed potent activity with MIC value of 2μg/ml, however, it lacked activity against several Gram-negative microbes with intact efflux systems, including E. coli BW25113 (wild-type strain). Combination of 6c with colistin partially restored its antibacterial activity against wild strains (MIC range, 8-16μg/ml against E. coli, K. pneumoniae, A. baumannii, and P. aeruginosa). 6c exhibited no cytotoxicity against two mammalian cell lines. Therefore, compound 6c represents a promising lead for further optimization to overcome Gram-negative resistance alone or in combination therapy. | ||
| 534 | |c 2019 | ||
| 650 | 4 | |a Antibiotic synergy | |
| 650 | 4 | |a Antimicrobial resistance | |
| 650 | 4 | |a Benzimidazole | |
| 650 | 4 | |a Gram-negative bacteria | |
| 650 | 4 | |a Phenotypic screening | |
| 700 | 1 | |a Abutaleb, Nader S. |e VerfasserIn |4 aut | |
| 700 | 1 | |a Milik, Sandra N. |e VerfasserIn |4 aut | |
| 700 | 1 | |a Li, Daoyi |e VerfasserIn |4 aut | |
| 700 | 1 | |a El-Baz, Karim |e VerfasserIn |4 aut | |
| 700 | 1 | |a Shalaby, Menna-Allah W. |e VerfasserIn |4 aut | |
| 700 | 1 | |a Al-Karaki, Rawan |e VerfasserIn |4 aut | |
| 700 | 1 | |a Nasr, Maha |e VerfasserIn |4 aut | |
| 700 | 1 | |a Klein, Christian D. |e VerfasserIn |0 (DE-588)1060644894 |0 (DE-627)800410157 |0 (DE-576)416768717 |4 aut | |
| 700 | 1 | |a Abouzid, Khaled A. M. |e VerfasserIn |4 aut | |
| 700 | 1 | |a Seleem, Mohamed N. |e VerfasserIn |4 aut | |
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