Drug Resistance Modulation in Staphylococcus Aureus, a New Biological Activity for Mesoionic Hydrochloride Compounds

被引:20
作者
de Oliveira, Cledualdo Soares [1 ]
Falcao-Silva, Vivyanne dos Santos [3 ]
Siqueira-Junior, Jose Pinto [3 ]
Harding, David Peter [1 ]
Lira, Bruno Freitas [1 ]
Fernandes Lorenzo, Jorge Goncalo [2 ]
Barbosa-Filho, Jose Maria [2 ]
de Athayde-Filho, Petronio Filgueiras [1 ]
机构
[1] Univ Fed Paraiba, Dept Chem, BR-58059 Joao Pessoa, PB, Brazil
[2] Univ Fed Paraiba, Pharmaceut Technol Lab, BR-58051 Joao Pessoa, PB, Brazil
[3] Univ Fed Paraiba, Dept Mol Biol, BR-58059 Joao Pessoa, PB, Brazil
关键词
mesoionic compounds; modulation of drug resistance; efflux pump inhibitor; MULTIDRUG-RESISTANCE; ABSORPTION;
D O I
10.3390/molecules16032023
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Two salts of the mesoionic compounds 1,4-diphenyl-5-(5-nitro-2-furanyl)-1,3,4thiadiazolium-2-thiol chloride (MC-1) and 4-phenyl-5-(5-nitro-2-furanyl)-1,3,4thiadiazolium-2-phenylamine chloride (MC-2) were synthesized utilizing 1,4-diphenyl-thiosemicarbazide and 5-nitro-2-furoyl chloride as starting materials. Their structures were characterized by IR, H-1-NMR, C-13-NMR and elemental analysis. These compounds were analyzed for their influence on the effectiveness of norfloxacin, tetracycline, and erythromycin (standard antibiotics) against resistant strains of Staphylococcus aureus. MC-1 and MC-2, at sub-inhibitory concentrations of 16 mu g/mL, favourably modulated the antibiotic activity of tetracycline by 16-and 32-fold, respectively (MIC), and that of erythromycin by 4-fold.
引用
收藏
页码:2023 / 2031
页数:9
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