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Título: | Discovery of niclosamide and its O-alkylamino-tethered derivatives as potent antibacterial agents against carbapenemase-producing and/or colistin resistant Enterobacteriaceae isolates |
Autor: | Xu, Jimin; Pachón-Ibáñez, M. E. CSIC ORCID; Cebrero-Cangueiro, Tania CSIC ORCID; Chen, Haiying; Sánchez-Céspedes, Javier CSIC ORCID | Palabras clave: | Niclosamide derivatives Antibacterial agents Carbapenemase-producing Enterobacteriaceae Colistin resistance Synergistic effects |
Fecha de publicación: | 1-jun-2019 | Editor: | Elsevier | Citación: | Bioorganic and Medicinal Chemistry Letters 29(11): 1399-1402 (2019) | Resumen: | Carbapenemase-producing Enterobacteriaceae (CPE) represents the most worrisome evolution of the antibiotic resistance crisis, which is almost resistant to most of available antibiotics. This situation is getting even worse particularly due to the recent emergence of colistin resistance. Herein, niclosamide, an FDA-approved traditional drug, and its novel O-alkylamino-tethered derivatives were discovered as new and potent antibacterial agents against carbapenemase-producing and/or colistin resistant Enterobacteriaceae isolates. Among these molecules, compound 10 (HJC0431) with 4-aminobutyl moiety showed the broad antibacterial activities, effective against 6 strains. In vitro checkerboard and time-kill course studies demonstrated the synergistic effects of the screened compounds with colistin against the corresponding strains with various degrees. | Versión del editor: | https://doi.org/10.1016/j.bmcl.2019.03.032 | URI: | http://hdl.handle.net/10261/202348 | DOI: | 10.1016/j.bmcl.2019.03.032 | E-ISSN: | 0960-894X |
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