Abstract
A series of related 3-hydroxypyridin-4-one hexadentate ligands have been synthesized. These chelators were found to possess a high affinity for iron(III), with a pFe value of about 30. As iron is a critical element to the survival of bacteria, these chelators were predicted to inhibit the growth of bacteria by disrupting bacterial iron absorption. Indeed, they were demonstrated to possess appreciable inhibitory activity against both Gram-positive and Gram-negative bacteria, and therefore, they have potential as antimicrobial agents. 1c and 1g were found to be particularly effective against Gram-negative species.
Graphical Abstract
A series of related 3-hydroxypyridin-4-one hexadentate ligands have been synthesized. These chelators were found to possess a high affinity for iron(III), and exhibit appreciable inhibitory activity against both Gram-positive and Gram-negative bacteria, and therefore, they have potential as antimicrobial agents.
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Acknowledgments
This research work was financially supported by the National Natural Science Foundation of China (No. 20972138), Ningbo Science and Technology Bureau of China (No. 2007C10066), Scientific Research Foundation for the Returned Overseas Chinese Scholars, State Education Ministry of China ([2009]1590), and Qianjiang Scholars Fund of Zhejiang Province (No. 2010R10051).
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Xie, YY., Liu, MS., Hu, PP. et al. Synthesis, physico-chemical properties, and antimicrobial evaluation of a new series of iron(III) hexadentate chelators. Med Chem Res 22, 2351–2359 (2013). https://doi.org/10.1007/s00044-012-0229-1
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DOI: https://doi.org/10.1007/s00044-012-0229-1