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| Verfasst von: | Dokla, Eman M. E. [VerfasserIn]  |
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| | Abutaleb, Nader S. [VerfasserIn] |
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| | Milik, Sandra N. [VerfasserIn] |
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| | Li, Daoyi [VerfasserIn] |
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| | El-Baz, Karim [VerfasserIn] |
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| | Shalaby, Menna-Allah W. [VerfasserIn] |
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| | Al-Karaki, Rawan [VerfasserIn] |
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| | Nasr, Maha [VerfasserIn] |
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| | Klein, Christian D. [VerfasserIn] |
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| | Abouzid, Khaled A. M. [VerfasserIn] |
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| | Seleem, Mohamed N. [VerfasserIn] |
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| Titel: | Development of benzimidazole-based derivatives as antimicrobial agents and their synergistic effect with colistin against gram-negative bacteria |
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| Verf.angabe: | 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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| E-Jahr: | 2020 |
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| Jahr: | [15 January 2020] |
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| Jahr des Originals: | 2019 |
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| Umfang: | 9 S. |
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| Illustrationen: | Diagramme |
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| Fussnoten: | Available online 5 November 2019 ; Gesehen am 02.04.2020 |
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| Titel Quelle: | Enthalten in: European journal of medicinal chemistry |
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| Ort Quelle: | Amsterdam [u.a.] : Elsevier Science, 1987 |
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| Jahr Quelle: | 2020 |
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| Band/Heft Quelle: | 186(2020) Artikel-Nummer 111850, Seite 1-9 |
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| ISSN Quelle: | 1768-3254 |
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| Abstract: | 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. |
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| DOI: | doi:10.1016/j.ejmech.2019.111850 |
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| URL: | Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.
Volltext: https://doi.org/10.1016/j.ejmech.2019.111850 |
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| | Volltext: http://www.sciencedirect.com/science/article/pii/S0223523419310025 |
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| | DOI: https://doi.org/10.1016/j.ejmech.2019.111850 |
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| Datenträger: | Online-Ressource |
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| Sprache: | eng |
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| Sach-SW: | Antibiotic synergy |
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| | Antimicrobial resistance |
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| | Benzimidazole |
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| | Gram-negative bacteria |
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| | Phenotypic screening |
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| K10plus-PPN: | 1693800756 |
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| Verknüpfungen: | → Zeitschrift |
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Development of benzimidazole-based derivatives as antimicrobial agents and their synergistic effect with colistin against gram-negative bacteria / Dokla, Eman M. E. [VerfasserIn]; [15 January 2020] (Online-Ressource)
