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

Molecules

Cledualdo Soares de Oliveira¹  Vivyanne Dos Santos Falcão-Silva¹  José Pinto Siqueira-Júnior¹  David Peter Harding¹  Bruno Freitas Lira¹  Jorge Gonçalo Fernandes Lorenzo¹  José Maria Barbosa-Filho¹ 

[1] ¹Department of Chemistry, Federal University of Paraíba, 58059, João Pessoa, PB, Brazil ²Laboratory of Pharmaceutical Technology, Federal University of Paraíba, 58051, João Pessoa, PB, Brazil ³Department of Molecular Biology, Federal University of Paraíba, 58059, João Pessoa, PB, Brazil

关键词: mesoionic compounds;    modulation of drug resistance;    efflux pump inhibitor;   

DOI  :  10.3390/molecules16032023

来源: mdpi

【 摘 要 】

Two salts of the mesoionic compounds 1,4-diphenyl-5-(5-nitro-2-furanyl)-1,3,4-thiadiazolium-2-thiol chloride (MC-1) and 4-phenyl-5-(5-nitro-2-furanyl)-1,3,4-thiadiazolium-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, ¹H-NMR, ¹³C-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 μg/mL, favourably modulated the antibiotic activity of tetracycline by 16- and 32-fold, respectively (MIC), and that of erythromycin by 4-fold.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.