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

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...

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Main Authors: Petrônio Filgueiras de Athayde-Filho, Cledualdo Soares de Oliveira, David Peter Harding, Bruno Freitas Lira, Jorge Gonçalo Fernandes Lorenzo, José Pinto Siqueira-Júnior, José Maria Barbosa-Filho, Vivyanne dos Santos Falcão-Silva
Format: Article
Language:English
Published: MDPI AG 2011-02-01
Series:Molecules
Subjects:
Online Access:http://www.mdpi.com/1420-3049/16/3/2023/
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author Petrônio Filgueiras de Athayde-Filho
Cledualdo Soares de Oliveira
David Peter Harding
Bruno Freitas Lira
Jorge Gonçalo Fernandes Lorenzo
José Pinto Siqueira-Júnior
José Maria Barbosa-Filho
Vivyanne dos Santos Falcão-Silva
author_facet Petrônio Filgueiras de Athayde-Filho
Cledualdo Soares de Oliveira
David Peter Harding
Bruno Freitas Lira
Jorge Gonçalo Fernandes Lorenzo
José Pinto Siqueira-Júnior
José Maria Barbosa-Filho
Vivyanne dos Santos Falcão-Silva
author_sort Petrônio Filgueiras de Athayde-Filho
collection DOAJ
description 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.
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spelling doaj.art-29ba3d93f3cb46eabacd4fcae0dca87a2022-12-21T20:56:16ZengMDPI AGMolecules1420-30492011-02-011632023203110.3390/molecules16032023Drug Resistance Modulation in Staphylococcus Aureus, a New Biological Activity for Mesoionic Hydrochloride CompoundsPetrônio Filgueiras de Athayde-FilhoCledualdo Soares de OliveiraDavid Peter HardingBruno Freitas LiraJorge Gonçalo Fernandes LorenzoJosé Pinto Siqueira-JúniorJosé Maria Barbosa-FilhoVivyanne dos Santos Falcão-SilvaTwo 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.http://www.mdpi.com/1420-3049/16/3/2023/mesoionic compoundsmodulation of drug resistanceefflux pump inhibitor
spellingShingle Petrônio Filgueiras de Athayde-Filho
Cledualdo Soares de Oliveira
David Peter Harding
Bruno Freitas Lira
Jorge Gonçalo Fernandes Lorenzo
José Pinto Siqueira-Júnior
José Maria Barbosa-Filho
Vivyanne dos Santos Falcão-Silva
Drug Resistance Modulation in Staphylococcus Aureus, a New Biological Activity for Mesoionic Hydrochloride Compounds
Molecules
mesoionic compounds
modulation of drug resistance
efflux pump inhibitor
title Drug Resistance Modulation in Staphylococcus Aureus, a New Biological Activity for Mesoionic Hydrochloride Compounds
title_full Drug Resistance Modulation in Staphylococcus Aureus, a New Biological Activity for Mesoionic Hydrochloride Compounds
title_fullStr Drug Resistance Modulation in Staphylococcus Aureus, a New Biological Activity for Mesoionic Hydrochloride Compounds
title_full_unstemmed Drug Resistance Modulation in Staphylococcus Aureus, a New Biological Activity for Mesoionic Hydrochloride Compounds
title_short Drug Resistance Modulation in Staphylococcus Aureus, a New Biological Activity for Mesoionic Hydrochloride Compounds
title_sort drug resistance modulation in staphylococcus aureus a new biological activity for mesoionic hydrochloride compounds
topic mesoionic compounds
modulation of drug resistance
efflux pump inhibitor
url http://www.mdpi.com/1420-3049/16/3/2023/
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