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Molecules 2018, 23(7), 1776; https://doi.org/10.3390/molecules23071776

A New Kind of Quinonic-Antibiotic Useful Against Multidrug-Resistant S. aureus and E. faecium Infections

1
Drug Development Laboratory, Faculty of Chemical and Pharmaceutical, Sciences, Universidad de Chile, Sergio Livingstone 1007, Santiago 8380492, Chile
2
Facultad de Medicina y Ciencia, Universidad San Sebastián, Lago, Panguipulli 1390, Puerto Montt 5501842, Chile
3
Laboratorio de Investigación en Agentes Antibacterianos (LIAA), Departamento de Microbiología, Facultad de Ciencias Biológicas, Universidad de Concepción, Concepción 4070386, Chile
4
Laboratorio de Estudios Cristalográficos, IACT (CSIC-UGR), Av. de las Palmeras 4, 18100 Armilla (Granada), Spain
5
Bioelectrochemistry Laboratory, Faculty of Chemical and Pharmaceutical, Sciences, Universidad de Chile, Santiago 8380492, Chile
6
Molecular Pharmacology and Toxicology Laboratory, Pharmacy Department, Faculty of Chemistry, Pontificia Universidad Católica de Chile; Santiago 7820436, Chile
7
Agents of bacterial meningitis laboratory, Instituto de Salud Pública de Chile, Santiago 7780050, Chile
8
Microbiology Unit, Clinical Laboratory, Clinical Hospital University of Chile; Santiago 8380456, Chile
9
Antibiotics Laboratory, Microbiology Program, Biomedical Sciences Institute, Faculty of Medicine, Universidad de Chile, Santiago 8380453, Chile
10
Nanobiotechnology and Nanotoxicology Laboratory, Faculty of Chemical and Pharmaceutical Sciences, Universidad de Chile, Santiago 8380494, Chile
11
Institute of Chemistry and Biochemistry, Faculty of Sciences, Universidad de Valparaíso, Playa Ancha, Valparaíso 2360102, Chile
12
Escuela de Quimica y Farmacia, Facultad de Medicina, Universidad Andres Bello, Quillota 980, Viña del Mar 2531015, Chile
13
Laboratory of Synthesis of Bioactive Heterocycles, Pharmacy Department, Faculty of Chemistry, Pontificia Universidad Católica de Chile; Santiago 7820436, Chile
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Received: 13 June 2018 / Revised: 11 July 2018 / Accepted: 17 July 2018 / Published: 19 July 2018
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Abstract

A rapid emergence of resistant bacteria is occurring worldwide, endangering the efficacy of antibiotics and reducing the therapeutic arsenal available for treatment of infectious diseases. In the present study, we developed a new class of compounds with antibacterial activity obtained by a simple, two step synthesis and screened the products for in vitro antibacterial activity against ATCC® strains using the broth microdilution method. The compounds exhibited minimum inhibitory concentrations (MIC) of 1–32 μg/mL against Gram-positive ATCC® strains. The structure–activity relationship indicated that the thiophenol ring is essential for antibacterial activity and the substituents on the thiophenol ring module, for antibacterial activity. The most promising compounds detected by screening were tested against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecium (VREF) clinical isolates. We found remarkable activity against VREF for compounds 7 and 16, were the MIC50/90 were 2/4 µg/mL and 4/4 µg/mL, respectively, while for vancomycin the MIC50/90 was 256/512 µg/mL. Neither compound affected cell viability in any of the mammalian cell lines at any of the concentrations tested. These in vitro data show that compounds 7 and 16 have an interesting potential to be developed as new antibacterial drugs against infections caused by VREF. View Full-Text
Keywords: quinonic-antibiotics; methicillin-resistant Staphylococcus aureus; vancomycin-resistant Enterococcus faecium; antibacterial activity quinonic-antibiotics; methicillin-resistant Staphylococcus aureus; vancomycin-resistant Enterococcus faecium; antibacterial activity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Campanini-Salinas, J.; Andrades-Lagos, J.; Gonzalez Rocha, G.; Choquesillo-Lazarte, D.; Bollo Dragnic, S.; Faúndez, M.; Alarcón, P.; Silva, F.; Vidal, R.; Salas-Huenuleo, E.; Kogan, M.; Mella, J.; Recabarren Gajardo, G.; Vásquez-Velásquez, D. A New Kind of Quinonic-Antibiotic Useful Against Multidrug-Resistant S. aureus and E. faecium Infections. Molecules 2018, 23, 1776.

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