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https://www.arca.fiocruz.br/handle/icict/51069
ENHANCEMENT OF ANTIBIOTIC ACTIVITY BY 1,8-NAPHTHYRIDINE DERIVATIVES AGAINST MULTI-RESISTANT BACTERIAL STRAINS
Author
Araújo-Neto, José B. de
Silva, Maria M. C. da
Tintino, Cícera D. de M. Oliveira
Begnini, Iêda M.
Rebelo, Ricardo A.
Silva, Luiz E. da
Mireski, Sandro L.
Nasato, Michele C.
Krautler, Maria I. L.
Ribeiro-Filho, Jaime
Siyadatpanah, Abolghasem
Wilairatana, Polrat
Coutinho, Henrique D. M.
Tintino, Saulo R.
Silva, Maria M. C. da
Tintino, Cícera D. de M. Oliveira
Begnini, Iêda M.
Rebelo, Ricardo A.
Silva, Luiz E. da
Mireski, Sandro L.
Nasato, Michele C.
Krautler, Maria I. L.
Ribeiro-Filho, Jaime
Siyadatpanah, Abolghasem
Wilairatana, Polrat
Coutinho, Henrique D. M.
Tintino, Saulo R.
Affilliation
Universidade Regional do Cariri. Laboratório de Microbiologia e Biologia Molecular. Fortaleza, CE, Brasil.
Universidade Regional do Cariri. Laboratório de Microbiologia e Biologia Molecular. Fortaleza, CE, Brasil.
Universidade Regional do Cariri. Laboratório de Microbiologia e Biologia Molecular. Fortaleza, CE, Brasil.
Universidade Regional de Blumenau. Departamento de Química. Blumenau, SC, Brasil.
Universidade Regional de Blumenau. Departamento de Química. Blumenau, SC, Brasil.
Universidade Federal do Paraná. Programa de Pós-Graduação em Desenvolvimento Territorial Sustentável – Setor Costeiro. Curitiba, PR, Brasil.
Universidade Regional de Blumenau. Departamento de Química. Blumenau, SC, Brasil.
Universidade Regional de Blumenau. Departamento de Química. Blumenau, SC, Brasil.
Universidade Regional de Blumenau. Departamento de Química. Blumenau, SC, Brasil.
Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil.
Ferdows School of Paramedical and Health. Birjand University of Medical Sciences. Birjand, Iran / Infectious Diseases Research Center. Birjand University of Medical Sciences. Birjand, Iran.
Department of Clinical Tropical Medicine. Faculty of Tropical Medicine. Mahidol University. Bangkok, Thailand.
Universidade Regional do Cariri. Laboratório de Microbiologia e Biologia Molecular. Fortaleza, CE, Brasil.
Universidade Regional do Cariri. Laboratório de Microbiologia e Biologia Molecular. Fortaleza, CE, Brasil.
Universidade Regional do Cariri. Laboratório de Microbiologia e Biologia Molecular. Fortaleza, CE, Brasil.
Universidade Regional do Cariri. Laboratório de Microbiologia e Biologia Molecular. Fortaleza, CE, Brasil.
Universidade Regional de Blumenau. Departamento de Química. Blumenau, SC, Brasil.
Universidade Regional de Blumenau. Departamento de Química. Blumenau, SC, Brasil.
Universidade Federal do Paraná. Programa de Pós-Graduação em Desenvolvimento Territorial Sustentável – Setor Costeiro. Curitiba, PR, Brasil.
Universidade Regional de Blumenau. Departamento de Química. Blumenau, SC, Brasil.
Universidade Regional de Blumenau. Departamento de Química. Blumenau, SC, Brasil.
Universidade Regional de Blumenau. Departamento de Química. Blumenau, SC, Brasil.
Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil.
Ferdows School of Paramedical and Health. Birjand University of Medical Sciences. Birjand, Iran / Infectious Diseases Research Center. Birjand University of Medical Sciences. Birjand, Iran.
Department of Clinical Tropical Medicine. Faculty of Tropical Medicine. Mahidol University. Bangkok, Thailand.
Universidade Regional do Cariri. Laboratório de Microbiologia e Biologia Molecular. Fortaleza, CE, Brasil.
Universidade Regional do Cariri. Laboratório de Microbiologia e Biologia Molecular. Fortaleza, CE, Brasil.
Abstract
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- aphthyridin-2-yl)-benzenesulfonamide. The antibioticmodulating 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 g/mL), they could decrease the MIC of these fluoroquinolones, indicating synergism was obtained from the association of the compounds. hese
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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