Antimicrobial activity of quinoline-based hydroxyimidazolium hybrids

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dc.citation.titleAntibioticses
dc.citation.volume8(4)es
dc.creatorInsuasty, Daniel
dc.creatorVidal, Oscar
dc.creatorBernal, Anthony
dc.creatorMarquez, Edgar
dc.creatorGuzman, Juan
dc.creatorInsuasty, Braulio
dc.creatorSvetaz, Laura
dc.creatorZacchino, Susana
dc.creatorPuerto, Gloria
dc.date.accessioned2020-12-16T21:37:42Z
dc.date.available2020-12-16T21:37:42Z
dc.date.issued2019-11-28
dc.descriptionEight quinoline-based hydroxyimidazolium hybrids 7aā€“h were prepared and evaluated in vitro against a panel of clinically important fungal and bacterial pathogens, including mycobacteria. Hybrid compounds 7cā€“d showed remarkable antifungal activity against Cryptococcus neoformans with a minimum inhibitory concentration (MIC) value of 15.6 Āµg/mL. Against other opportunistic fungi such as Candida spp. and Aspergillus spp., these hybrids showed MIC values of 62.5 Āµg/mL. Regarding their antibacterial activity, all the synthetic hybrids demonstrated little inhibition of Gram-negative bacteria (MIC ā‰„50 Āµg/mL), however, hybrid 7b displayed >50% inhibition against Klebsiella pneumoniae at 20 Āµg/mL and full inhibition at 50 Āµg/mL. Moreover, this hybrid was shown to be a potent anti-staphylococcal molecule, with a MIC value of 2 Āµg/mL (5 ĀµM). In addition, hybrid 7h also demonstrated inhibition of Staphylococcus aureus at 20 Āµg/mL (47 ĀµM). Hybrids 7a and 7b were the most potent against Mycobacterium tuberculosis H37Rv with MIC values of 20 and 10 Āµg/mL (46 and 24 ĀµM), respectively. The 7b hybrid demonstrated high selectivity in killing S. aureus and M. tuberculosis H37Rv in comparison with mammalian cells (SI >20), and thus it can be considered a hit molecule for mechanism of action studies and the exploration of related chemical space.es
dc.descriptionPara citar este articulo: Insuasty, D.; Vidal, O.; Bernal, A.; Marquez, E.; Guzman, J.; Insuasty, B.; Quiroga, J.; Svetaz, L.; Zacchino, S.; Puerto, G.; Abonia, R. Antimicrobial Activity of Quinoline-Based Hydroxyimidazolium Hybrids. Antibiotics 2019, 8, 239.
dc.description.filFil: Insuasty, Daniel. Universidad del Norte. Departamento de QuĆ­mica y BiologĆ­a; Colombia.es
dc.description.filFil: Vidal, Oscar. Universidad del Norte. Departamento de QuĆ­mica y BiologĆ­a; Colombia.es
dc.description.filFil: Bernal, Anthony. Universidad del Norte. Departamento de QuĆ­mica y BiologĆ­a; Colombia.es
dc.description.filFil: Marquez, Edgar. Universidad del Norte. Departamento de QuĆ­mica y BiologĆ­a; Colombia.es
dc.description.filFil: Guzman, Juan. Justus Liebig University Giessen. Institute for Insect Biotechnology; Germany.es
dc.description.filFil: Insuasty, Braulio. Universidad del Valle. Facultad de Ciencias Naturales y Exactas. Departamento de QuĆ­mica. Grupo de InvestigaciĆ³n de Compuestos HeterocĆ­clicos; Colombia.es
dc.description.filFil: Svetaz, Laura. Universidad Nacional de Rosario. Facultad de Ciencias Bioquƭmicas y FarmacƩuticas. Ɓrea Farmacognosia; Argentina.es
dc.description.filFil: Zacchino, Susana. Universidad Nacional de Rosario. Facultad de Ciencias Bioquƭmicas y FarmacƩuticas. Ɓrea Farmacognosia; Argentina.es
dc.description.filFil: Puerto, Gloria. Instituto Nacional de Salud. Laboratorio de Micobacterias; Colombia.es
dc.description.sponsorshipAgencia Nacional de PromociĆ³n CientĆ­fica y TecnolĆ³gica (ANPCyT): PICT2016-1833es
dc.description.sponsorshipUniversidad Nacional de Rosario (UNR)es
dc.description.sponsorshipDepartamento Administrativo de Ciencia, TecnologĆ­a e InnovaciĆ³n (Colciencias)es
dc.description.sponsorshipUniversidad del Vallees
dc.description.sponsorshipUniversidad del Nortees
dc.formatapplication/pdf
dc.format.extent1-11es
dc.identifier.issn2079-6382es
dc.identifier.urihttp://hdl.handle.net/2133/19489
dc.language.isoenges
dc.publisherMDPIes
dc.relation.publisherversionhttps://doi.org/10.3390/antibiotics8040239es
dc.relation.publisherversionhttps://www.mdpi.com/2079-6382/8/4/239#citees
dc.rightsopenAccesses
dc.rights.holderUniversidad Nacional de Rosarioes
dc.rights.holderInsuasty, Danieles
dc.rights.holderVidal, Oscares
dc.rights.holderBernal, Anthonyes
dc.rights.holderMarquez, Edgares
dc.rights.holderGuzman, Juanes
dc.rights.holderInsuasty, Braulioes
dc.rights.holderSvetaz, Lauraes
dc.rights.holderZacchino, Susanaes
dc.rights.textAttribution 4.0 International (CC BY 4.0)es
dc.rights.urihttps://creativecommons.org/licenses/by/4.0/*
dc.subjectQuinoline-based Hydroxyimidazolium Hybridses
dc.subjectAntimicrobial Activityes
dc.subjectAntifungal Activityes
dc.subjectTuberculosises
dc.subjectCytotoxicityes
dc.titleAntimicrobial activity of quinoline-based hydroxyimidazolium hybridses
dc.typearticle
dc.typeartĆ­culo
dc.typepublishedVersion
dc.type.collectionarticulo
dc.type.versionpublishedVersiones

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