Vancomycin-Teixobactin Conjugates.

ABSTRACT: Vancomycin continues to be a widely used antibiotic of last resort in treating drug-resistant pathogens despite the emergence of vancomycin-resistant strains such as vancomycin-resistant Enterococci (VRE). This communication reports that conjugation of vancomycin to a second antibiotic that targets a different region of lipid II enhances and rescues its antibiotic activity. Conjugation of vancomycin to a minimal teixobactin pharmacophore in which residues 1-6 are replaced with an aromatic amide results in substantial enhancement in activity over the individual components or mixtures thereof. Three conjugates with minimum inhibitory concentrations (MICs) of 0.5 μg/mL against methicillin-resistant Staphylococcus aureus (MRSA) and 0.063-0.125 μg/mL against methicillin-susceptibl

SUBMITTER: Padilla MSTL 

PROVIDER: S-EPMC11869278 | biostudies-literature | 2025 Feb

REPOSITORIES: biostudies-literature