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Antimicrobial Activity of Quinoline-Based Hydroxyimidazolium Hybrids

Departamento de Química y Biología, Universidad del Norte, Km 5 vía Puerto Colombia, Barranquilla 081007, Colombia
Institute for Insect Biotechnology, Justus-Liebig-University of Giessen, 35392 Giessen, Germany
Research Group of Heterocyclic Compounds, Department of Chemistry, Universidad del Valle, A. A. Cali 25360, Colombia
Área Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, Rosario 2000, Argentina
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.

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.

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.

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