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

Antibacterial small molecules that potently inhibit Staphylococcus aureus lipoteichoic acid biosynthesis. ChemMedChem. 2019 Apr 02;: Authors: Sintim HO, Naclerio GA, Karanja CW, Opoku-Temeng C Abstract 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. PMID: 30939229 [PubMed - as supplied by publisher]
Source: ChemMedChem - Category: Chemistry Authors: Tags: ChemMedChem Source Type: research