Publication: Enhancement of antibiotic activity by 1,8-naphthyridine derivatives against multi-resistant bacterial strains
Issued Date
2021-12-01
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14203049
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2-s2.0-85121150091
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Mahidol University
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SCOPUS
Bibliographic Citation
Molecules. Vol.26, No.23 (2021)
Suggested Citation
José B. de Araújo-Neto, Maria M.C. da Silva, Cícera D.de M. Oliveira-Tintino, Iêda M. Begnini, Ricardo A. Rebelo, Luiz E. da Silva, Sandro L. Mireski, Michele C. Nasato, Maria I.L. Krautler, Jaime Ribeiro-Filho, Abolghasem Siyadatpanah, Polrat Wilairatana, Henrique D.M. Coutinho, Saulo R. Tintino Enhancement of antibiotic activity by 1,8-naphthyridine derivatives against multi-resistant bacterial strains. Molecules. Vol.26, No.23 (2021). doi:10.3390/molecules26237400 Retrieved from: https://repository.li.mahidol.ac.th/handle/123456789/75901
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Title
Enhancement of antibiotic activity by 1,8-naphthyridine derivatives against multi-resistant bacterial strains
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Abstract
The search for new antibacterial agents has become urgent due to the exponential growth of bacterial resistance to antibiotics. Nitrogen-containing heterocycles such as 1,8-naphthyridine derivatives have been shown to have excellent antimicrobial properties. Therefore, the purpose of this study was to evaluate the antibacterial and antibiotic-modulating activities of 1,8-naphthyridine derivatives against multi-resistant bacterial strains. The broth microdilution method was used to determine the minimum inhibitory concentration (MIC) of the following compounds: 7-acetamido-1,8-naphthyridin-4(1H)-one and 3-trifluoromethyl-N-(5-chloro-1,8-naphthyridin-2-yl)-benzenesulfonamide. The antibiotic-modulating activity was analyzed using subinhibitory concentrations (MIC/8) of these compounds in combination with norfloxacin, ofloxacin, and lomefloxacin. Multi-resistant strains of Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus were used in both tests. Although the compounds had no direct antibacterial activity (MIC ≥ 1.024 µg/mL), they could decrease the MIC of these fluoroquinolones, indicating synergism was obtained from the association of the compounds. These results suggest the existence of a structure–activity relationship in this group of compounds with regard to the modulation of antibiotic activity. Therefore, we conclude that 1,8-naphthyridine derivatives potentiate the activity of fluoroquinolone antibiotics against multi-resistant bacterial strains, and thereby interesting candidates for the development of drugs against bacterial infections caused by multidrug resistant strains.