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

AutorCampanini-Salinas, Javier; Andrades-Lagos, Juan; Gonzalez Rocha, Gerardo; Choquesillo-Lazarte, Duane ; Bollo Dragnic, Soledad; Faúndez, Mario; Alarcón, Pedro; Silva, Francisco; Vidal, Roberto; Salas-Huenuleo, Edison; Kogan, Marcelo; Mella, Jaime; Recabarren Gajardo, Gonzalo; Vásquez-Velásquez, David
Fecha de publicación19-jul-2018
EditorMultidisciplinary Digital Publishing Institute
CitaciónMolecules 23 (7): 1776 (2018)
ResumenA 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<sup>&reg;</sup> strains using the broth microdilution method. The compounds exhibited minimum inhibitory concentrations (MIC) of 1&ndash;32 &mu;g/mL against Gram-positive ATCC<sup>&reg;</sup> strains. The structure&ndash;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 <i>Staphylococcus aureus</i> (MRSA) and vancomycin-resistant <i>Enterococcus faecium</i> (VREF) clinical isolates. We found remarkable activity against VREF for compounds <b>7</b> and <b>16</b>, were the MIC<sub>50/90</sub> were 2/4 &micro;g/mL and 4/4 &micro;g/mL, respectively, while for vancomycin the MIC<sub>50/90</sub> was 256/512 &micro;g/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 <b>7</b> and <b>16</b> have an interesting potential to be developed as new antibacterial drugs against infections caused by VREF.
URIhttp://hdl.handle.net/10261/167940
Identificadoresdoi: 10.3390/molecules23071776
Aparece en las colecciones: Colección MDPI
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