Antibacterial small molecules that potently inhibit Staphylococcus aureus lipoteichoic acid biosynthesis.

08:00 EDT 2nd April 2019 | BioPortfolio

Summary of "Antibacterial small molecules that potently inhibit Staphylococcus aureus lipoteichoic acid biosynthesis."

The rise of antibiotic resistance, especially in staphylococcus aureus, and the increasing death rate due to multi-resistant bacteria have been well documented. The need for new chemical entities and/or the identification of novel targets for antibacterial drug development is high. Lipoteichoic acid (LTA), a membrane attached anionic polymer, is important for the growth and virulence of many Gram-positive bacteria and interest has been high in the discovery of LTA biosynthesis inhibitors. Thus far only a handful of LTA biosynthesis inhibitors have been described with moderate (MIC = 5.34 µg/mL) to low (MIC = 1024 µg/mL) activities against S. aureus. Here we describe the identification of novel compounds that potently inhibit LTA biosynthesis in S. aureus, displaying impressive antibacterial activities (MIC as low as 0.25 µg/mL) against methicillin-resistant S. aureus (MRSA). Under similar in-vitro assay conditions, these compounds are 4X more potent than vancomycin and 8X more potent than Linezolid against MRSA.


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This article was published in the following journal.

Name: ChemMedChem
ISSN: 1860-7187


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