Antimicrobial activity of quinoline-based hydroxyimidazolium hybrids
No Thumbnail Available
Date
2019-11-28
Journal Title
Journal ISSN
Volume Title
Publisher
MDPI
Abstract
Description
Eight quinoline-based hydroxyimidazolium hybrids 7aāh were prepared and evaluated
in vitro against a panel of clinically important fungal and bacterial pathogens, including mycobacteria.
Hybrid compounds 7cād 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.
Para 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.
Para 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.
Keywords
Quinoline-based Hydroxyimidazolium Hybrids, Antimicrobial Activity, Antifungal Activity, Tuberculosis, Cytotoxicity