Antimicrobial activity of quinoline-based hydroxyimidazolium hybrids

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 inh...

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Autores principales: Insuasty, Daniel, Vidal, Oscar, Bernal, Anthony, Marquez, Edgar, Guzman, Juan, Insuasty, Braulio, Svetaz, Laura, Zacchino, Susana, Puerto, Gloria
Formato: article artículo publishedVersion
Lenguaje:Inglés
Publicado: MDPI 2020
Materias:
Quinoline-based Hydroxyimidazolium Hybrids
Antimicrobial Activity
Antifungal Activity
Tuberculosis
Cytotoxicity
Acceso en línea:http://hdl.handle.net/2133/19489
http://hdl.handle.net/2133/19489
Aporte de:
Repositorio Hipermedial de la Universidad Nacional de Rosario (UNR) de Universidad Nacional de Rosario
id I15-R121-2133-19489
record_format dspace
institution Universidad Nacional de Rosario
institution_str I-15
repository_str R-121
collection Repositorio Hipermedial de la Universidad Nacional de Rosario (UNR)
language Inglés
orig_language_str_mv eng
topic Quinoline-based Hydroxyimidazolium Hybrids
Antimicrobial Activity
Antifungal Activity
Tuberculosis
Cytotoxicity
spellingShingle Quinoline-based Hydroxyimidazolium Hybrids
Antimicrobial Activity
Antifungal Activity
Tuberculosis
Cytotoxicity
Insuasty, Daniel
Vidal, Oscar
Bernal, Anthony
Marquez, Edgar
Guzman, Juan
Insuasty, Braulio
Svetaz, Laura
Zacchino, Susana
Puerto, Gloria
Antimicrobial activity of quinoline-based hydroxyimidazolium hybrids
topic_facet Quinoline-based Hydroxyimidazolium Hybrids
Antimicrobial Activity
Antifungal Activity
Tuberculosis
Cytotoxicity
description 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.
format article
artículo
publishedVersion
author Insuasty, Daniel
Vidal, Oscar
Bernal, Anthony
Marquez, Edgar
Guzman, Juan
Insuasty, Braulio
Svetaz, Laura
Zacchino, Susana
Puerto, Gloria
author_facet Insuasty, Daniel
Vidal, Oscar
Bernal, Anthony
Marquez, Edgar
Guzman, Juan
Insuasty, Braulio
Svetaz, Laura
Zacchino, Susana
Puerto, Gloria
author_sort Insuasty, Daniel
title Antimicrobial activity of quinoline-based hydroxyimidazolium hybrids
title_short Antimicrobial activity of quinoline-based hydroxyimidazolium hybrids
title_full Antimicrobial activity of quinoline-based hydroxyimidazolium hybrids
title_fullStr Antimicrobial activity of quinoline-based hydroxyimidazolium hybrids
title_full_unstemmed Antimicrobial activity of quinoline-based hydroxyimidazolium hybrids
title_sort antimicrobial activity of quinoline-based hydroxyimidazolium hybrids
publisher MDPI
publishDate 2020
url http://hdl.handle.net/2133/19489
http://hdl.handle.net/2133/19489
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