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dc.contributor.author
Insuasty, Daniel
dc.contributor.author
Vidal, Oscar
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Bernal, Anthony
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Marquez, Edgar
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Guzman, Juan
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Insuasty, Braulio
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Quiroga, Jairo
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Svetaz, Laura Andrea
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Zacchino, Susana Alicia Stella
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Puerto, Gloria
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Abonia, Rodrigo
dc.date.available
2022-03-31T19:27:21Z
dc.date.issued
2019-11
dc.identifier.citation
Insuasty, Daniel; Vidal, Oscar; Bernal, Anthony; Marquez, Edgar; Guzman, Juan; et al.; Antimicrobial Activity of Quinoline-Based Hydroxyimidazolium Hybrids; MDPI; Antibiotics; 8; 4; 11-2019; 1-11
dc.identifier.issn
2079-6382
dc.identifier.uri
http://hdl.handle.net/11336/154137
dc.description.abstract
Eight quinoline-based hydroxyimidazolium hybrids 7a–h were prepared and evaluated in vitro against a panel of clinically important fungal and bacterial pathogens, including mycobacteria. Hybrid compounds 7c–d showed remarkable antifungal activity against Cryptococcus neoformans with a minimum inhibitory concentration (MIC) value of 15.6 µg/mL. Against other opportunistic fungi such as Candida spp. and Aspergillus spp., these hybrids showed MIC values of 62.5 µg/mL. Regarding their antibacterial activity, all the synthetic hybrids demonstrated little inhibition of Gram-negative bacteria (MIC ≥50 µg/mL), however, hybrid 7b displayed >50% inhibition against Klebsiella pneumoniae at 20 µg/mL and full inhibition at 50 µg/mL. Moreover, this hybrid was shown to be a potent anti-staphylococcal molecule, with a MIC value of 2 µg/mL (5 µM). In addition, hybrid 7h also demonstrated inhibition of Staphylococcus aureus at 20 µg/mL (47 µM). Hybrids 7a and 7b were the most potent against Mycobacterium tuberculosis H37Rv with MIC values of 20 and 10 µg/mL (46 and 24 µM), 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.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
MDPI
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by/2.5/ar/
dc.subject
ANTIFUNGAL ACTIVITY
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ANTIMICROBIAL ACTIVITY
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CYTOTOXICITY
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QUINOLINE-BASED HYDROXYIMIDAZOLIUM HYBRIDS
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TUBERCULOSIS
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Química Orgánica
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Ciencias Químicas
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CIENCIAS NATURALES Y EXACTAS
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dc.title
Antimicrobial Activity of Quinoline-Based Hydroxyimidazolium Hybrids
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2022-03-16T12:38:57Z
dc.identifier.eissn
2079-6382
dc.journal.volume
8
dc.journal.number
4
dc.journal.pagination
1-11
dc.journal.pais
Suiza
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dc.journal.ciudad
Basilea
dc.description.fil
Fil: Insuasty, Daniel. Universidad del Norte; Colombia
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Fil: Vidal, Oscar. Universidad del Norte; Colombia
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Fil: Bernal, Anthony. Universidad del Norte; Colombia
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Fil: Marquez, Edgar. Universidad del Norte; Colombia
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Fil: Guzman, Juan. Justus Liebig Universitat Giessen; Alemania
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Fil: Insuasty, Braulio. Universidad del Valle; Colombia
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Fil: Quiroga, Jairo. Universidad del Valle; Colombia
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Fil: Svetaz, Laura Andrea. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; Argentina
dc.description.fil
Fil: Zacchino, Susana Alicia Stella. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; Argentina
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Fil: Puerto, Gloria. Instituto Nacional de Salud; Colombia
dc.description.fil
Fil: Abonia, Rodrigo. Universidad del Valle; Colombia
dc.journal.title
Antibiotics
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://www.mdpi.com/2079-6382/8/4/239
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/https://dx.doi.org/10.3390/antibiotics8040239
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