Abstract
Two series of furan derivatives bearing a rhodanine moiety (4a–l and 5a–l) have been synthesized, characterized, and evaluated for their antibacterial activity. The majority of these compounds showed potent levels of inhibitory activity against a variety of different Gram-positive bacteria, including multidrug-resistant clinical isolates, with minimum inhibitory concentration (MIC) values in the range of 2–16 μg/mL. In particular, compound 4l was found to be the most potent of the synthesized compounds against the multidrug-resistant strains, with a MIC value of 2 or 4 μg/mL. None of the compounds exhibited any activity against the Gram-negative bacteria Escherichia coli 1356 at 64 μg/mL. An examination of the cytotoxicities of these agents revealed that they displayed low levels of toxicity toward HeLa cells. All of the compounds synthesized in the current paper were characterized by 1H and 13C NMR, infrared, and mass spectroscopy.
Graphical Abstract
Two novel series of furan derivatives bearing a rhodanine moiety were synthesized, and evaluated for their antibacterial activity. Compounds 4l and 5a presented high potency against several multidrug-resistant clinical isolates.
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This work was supported by the National Science Foundation of China (Grant Nos. 20962021 and 81260468).
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Che, J., Zheng, CJ., Song, MX. et al. Synthesis and antibacterial evaluation of furan derivatives bearing a rhodanine moiety. Med Chem Res 23, 426–435 (2014). https://doi.org/10.1007/s00044-013-0648-7
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DOI: https://doi.org/10.1007/s00044-013-0648-7