Abstract
The synthesis and screening of several fusaric acid (FA) and analogues against five common clinical pathogens (gram-positive and gram-negative) and in vitro hemolytic activity assay in human red blood cells, for the first time, were reported. The biological results reveal that FA and its analogues exhibited moderate antimicrobial activities. Compounds 2–5 and 7 showed growth inhibitory activity in gram-positive bacteria. Compounds 6 and 9 showed growth inhibitory activity in both gram-positive and gram-negative bacteria. None of the compounds induce hemolysis, which is potent for future drug development on this template. In addition, the structure–activity relationship and docking studies are discussed.
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Acknowledgements
This research is funded by The PHENIKAA University Foundation for Science and Technology Development. The authors would like to thank Prof. Niels Frimodt-Møller, Department of Clinical Microbiology, Rigshospitalet, Københavns Universitet, Denmark for hemolytic activity assay. We would like to thank Prof. John Nielsen, Department of Drug Design and Pharmacology, Københavns Universitet, Denmark for essential support at an early stage of the fusaric acid project.
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Thanh, T.T., Quoc, T.N. & Xuan, H.L. Fusaric acid and derivatives as novel antimicrobial agents. Med Chem Res 29, 1689–1696 (2020). https://doi.org/10.1007/s00044-020-02596-3
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DOI: https://doi.org/10.1007/s00044-020-02596-3