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 Andrea
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, Laura Andrea es
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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