Synthesis and Evaluation of Troponoids as a New Class of Antibiotics.

ABSTRACT: Novel antibiotics are urgently needed. The troponoids [tropones, tropolones, and α-hydroxytropolones (α-HT)] can have anti-bacterial activity. We synthesized or purchased 92 troponoids and evaluated their antibacterial activities against Staphylococcus aureus, Escherichia coli, Acinetobacter baumannii, and Pseudomonas aeruginosa. Preliminary hits were assessed for minimum inhibitory concentrations (MIC₈₀) and cytotoxicity (CC₅₀) against human hepatoma cells. Sixteen troponoids inhibited S. aureus/E. coli/A. baumannii growth by ≥80% growth at <30 μM with CC₅₀ values >50 μM. Two selected tropolones (63 and 285) inhibited 18 methicillin-resistant S. aureus (MRSA) strains with similar MIC

SUBMITTER: Cao F 

PROVIDER: S-EPMC6275967 | biostudies-literature | 2018 Nov

REPOSITORIES: biostudies-literature