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Synthesis and Evaluation of Troponoids as a New Class of Antibiotics #MMPMID30533576
Cao F; Orth C; Donlin MJ; Adegboyega P; Meyers MJ; Murelli RP; Elagawany M; Elgendy B; Tavis JE
ACS Omega 2018[Nov]; 3 (11): 15125-15133 PMID30533576show ga
Novel antibiotics are urgently needed. The troponoids [tropones, tropolones, and alpha-hydroxytropolones (alpha-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 (MIC(80)) and cytotoxicity (CC(50)) against human hepatoma cells. Sixteen troponoids inhibited S. aureus/E. coli/A. baumannii growth by >/=80% growth at <30 muM with CC(50) values >50 muM. Two selected tropolones (63 and 285) inhibited 18 methicillin-resistant S. aureus (MRSA) strains with similar MIC(80) values as against a reference strain. Two selected thiotropolones (284 and 363) inhibited multidrug-resistant (MDR) E. coli with MIC(80) =30 muM. One alpha-HT (261) inhibited MDR-A. baumannii with MIC(80) =30 muM. This study opens new avenues for development of novel troponoid antibiotics to address the critical need to combat MDR bacterial infections.