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Molecules 2011, 16(3), 2023-2031; doi:10.3390/molecules16032023

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

1
Department of Chemistry, Federal University of Paraíba, 58059, João Pessoa, PB, Brazil
2
Laboratory of Pharmaceutical Technology, Federal University of Paraíba, 58051, João Pessoa, PB, Brazil
3
Department of Molecular Biology, Federal University of Paraíba, 58059, João Pessoa, PB, Brazil
*
Author to whom correspondence should be addressed.
Received: 25 January 2011 / Revised: 19 February 2011 / Accepted: 22 February 2011 / Published: 28 February 2011
(This article belongs to the Special Issue Advances in Heterocyclic Chemistry)
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Abstract

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.
Keywords: mesoionic compounds; modulation of drug resistance; efflux pump inhibitor mesoionic compounds; modulation of drug resistance; efflux pump inhibitor
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MDPI and ACS Style

Soares de Oliveira, C.; Dos Santos Falcão-Silva, V.; Siqueira-Júnior, J.P.; Harding, D.P.; Lira, B.F.; Lorenzo, J.G.F.; Barbosa-Filho, J.M.; Filgueiras de Athayde-Filho, P. Drug Resistance Modulation in Staphylococcus Aureus, a New Biological Activity for Mesoionic Hydrochloride Compounds. Molecules 2011, 16, 2023-2031.

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