Synthesis and Evaluation of Troponoids as a New Class
of Antibiotics
Posted on 2018-11-08 - 18:37
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.
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Cao, Feng; Orth, Cari; J. Donlin, Maureen; Adegboyega, Patrick; Meyers, Marvin J.; Murelli, Ryan P.; et al. (2018). Synthesis and Evaluation of Troponoids as a New Class
of Antibiotics. ACS Publications. Collection. https://doi.org/10.1021/acsomega.8b01754
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AUTHORS (9)
FC
Feng Cao
CO
Cari Orth
MJ
Maureen J. Donlin
PA
Patrick Adegboyega
MM
Marvin J. Meyers
RM
Ryan P. Murelli
ME
Mohamed Elagawany
BE
Bahaa Elgendy
JE
John E. Tavis
KEYWORDS
CC 5018 methicillin-resistant SAntibiotics Novel antibioticsMDR-AAcinetobacter baumanniianti-bacterial activityMIC 80New ClassMIC 80 valuesα- HT92 troponoidsPreliminary hitsEscherichia colireference straintropolonenovel troponoid antibioticsStaphylococcus aureushepatoma cellsMRSAPseudomonas aeruginosacombat MDR