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Article

Antimicrobial Activity of Quinoline-Based Hydroxyimidazolium Hybrids

1
Departamento de Química y Biología, Universidad del Norte, Km 5 vía Puerto Colombia, Barranquilla 081007, Colombia
2
Institute for Insect Biotechnology, Justus-Liebig-University of Giessen, 35392 Giessen, Germany
3
Research Group of Heterocyclic Compounds, Department of Chemistry, Universidad del Valle, A. A. Cali 25360, Colombia
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Área Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, Rosario 2000, Argentina
5
Laboratorio de Micobacterias, Instituto Nacional de Salud, Bogotá 111321, Colombia
*
Authors to whom correspondence should be addressed.
Received: 25 October 2019 / Revised: 15 November 2019 / Accepted: 19 November 2019 / Published: 28 November 2019
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. View Full-Text
Keywords: quinoline-based hydroxyimidazolium hybrids; antimicrobial activity; antifungal activity; tuberculosis; cytotoxicity quinoline-based hydroxyimidazolium hybrids; antimicrobial activity; antifungal activity; tuberculosis; cytotoxicity
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MDPI and ACS Style

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. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics8040239

AMA Style

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(4):239. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics8040239

Chicago/Turabian Style

Insuasty, Daniel, Oscar Vidal, Anthony Bernal, Edgar Marquez, Juan Guzman, Braulio Insuasty, Jairo Quiroga, Laura Svetaz, Susana Zacchino, Gloria Puerto, and Rodrigo Abonia. 2019. "Antimicrobial Activity of Quinoline-Based Hydroxyimidazolium Hybrids" Antibiotics 8, no. 4: 239. https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics8040239

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