Synthetic macrolides overcoming MLS_BK-resistant pathogens.

ABSTRACT: Conventional macrolide-lincosamide-streptogramin B-ketolide (MLS_BK) antibiotics are unable to counter the growing challenge of antibiotic resistance that is conferred by the constitutive methylation of rRNA base A2058 or its G2058 mutation, while the presence of unmodified A2058 is crucial for high selectivity of traditional MLS_BK in targeting pathogens over human cells. The absence of effective modes of action reinforces the prevailing belief that constitutively antibiotic-resistant Staphylococcus aureus remains impervious to existing macrolides including telithromycin. Here, we report the design and synthesis of a novel series of macrolides, featuring the strategic fusion of ketolide and quinolone moieties. Our effort led to the discovery of two potent compounds, MC

SUBMITTER: Ma CX 

PROVIDER: S-EPMC11239830 | biostudies-literature | 2024 Jul

REPOSITORIES: biostudies-literature