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

Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
Javier Campanini-SalinasDavid Vásquez-Velásquez

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 vitr...Continue Reading

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Citations

Nov 28, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Jong Min OhHoon Kim
May 28, 2020·Folia Microbiologica·Emel Mataracı KaraAmaç Fatih Tuyun
Jun 3, 2021·Antibiotics·Javier Campanini-SalinasDavid Vásquez-Velásquez

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Methods Mentioned

BETA
X-ray
column chromatography

Software Mentioned

SADABS
APEX3
ChemDraw Ultra
GraphPad Prism

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An antifungal, also known as an antimycotic medication, is a pharmaceutical fungicide or fungistatic used to treat and prevent mycosis such as athlete's foot, ringworm, candidiasis, cryptococcal meningitis, and others. Discover the latest research on antifungals here.