Multi-Halogenated Indoles as Antimicrobial and Antivirulence Agents Against Drug-Resistant Staphylococcus aureus.

ABSTRACT: The emergence of multidrug-resistant Staphylococcus aureus requires the development of novel agents that can target both planktonic cells and persistent biofilms. In this study, a library of multi-halogenated indoles was evaluated for antibacterial, antibiofilm and antivirulence activities against S. aureus including methicillin-resistant strains. Two lead compounds, 6-bromo-4-iodoindole and 4-bromo-6-chloroindole, exhibited potent bactericidal activity (MIC = 20-30 μg/mL) comparable to the antibiotic gentamicin, effectively inhibited biofilm formation and persister formation and suppressed key virulence haemolysis. These effects were associated with intracellular ROS generation and transcriptional downregulation of quorum-sensing genes of agrA and RNAIII and virulence genes of hla and nuc

SUBMITTER: Sim M 

PROVIDER: S-EPMC12673945 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature