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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 MIC80 values as against a reference strain. Two selected thiotropolones (284 and 363) inhibited multidrug-resistant (MDR) E. coli with MIC80 ≤30 μM. One α-HT (261) inhibited MDR-A. baumannii with MIC80 ≤30 μM. This study opens new avenues for development of novel troponoid antibiotics to address the critical need to combat MDR bacterial infections.

SUBMITTER: Cao F 

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

REPOSITORIES: biostudies-literature

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

Cao Feng F   Orth Cari C   Donlin Maureen J MJ   Adegboyega Patrick P   Meyers Marvin J MJ   Murelli Ryan P RP   Elagawany Mohamed M   Elgendy Bahaa B   Tavis John E JE  

ACS omega 20181108 11

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 <i>Staphylococcus aureus</i>, <i>Escherichia coli</i>, <i>Acinetobacter baumannii,</i> and <i>Pseudomonas aeruginosa</i>. Preliminary hits were assessed for minimum inhibitory concentrations (MIC<sub>80</sub>) and cytotoxicity (CC<sub>50</sub>) against human hep  ...[more]

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