期刊
MOLECULES
卷 26, 期 23, 页码 -出版社
MDPI
DOI: 10.3390/molecules26237400
关键词
naphthyridine; naphthyridinone; fluoroquinolones; bacterial resistance; synergism
资金
- National Council of Scientific and Technological Development (CNPq) [150456/2018-2, 406685/2018-5]
- Coordination for the Improvement of Higher Education Personnel (CAPES) [001]
- Cearense Foundation for Scientific and Technological Development Support (FUNCAP)
- Financier of Studies and Projects-Brazil (FINEP)
This study evaluated the antibacterial and antibiotic-modulating activities of 1,8-naphthyridine derivatives against multi-resistant bacterial strains. While the compounds themselves had no direct antibacterial activity, they were able to potentiate the activity of fluoroquinolone antibiotics, indicating a potential for synergism in combating multidrug resistant bacterial infections.
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 mu g/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.
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