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Synthesis and antibacterial evaluation of furan derivatives bearing a rhodanine moiety

Authors :
Ming-Xia Song
Jian Che
Liang-Peng Sun
Yan Wu
Yin-Jing Li
Yi Liu
Chang-Ji Zheng
Hu-Ri Piao
Ya-Jing Bi
Source :
Medicinal Chemistry Research. 23:426-435
Publication Year :
2013
Publisher :
Springer Science and Business Media LLC, 2013.

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. 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.

Details

ISSN :
15548120 and 10542523
Volume :
23
Database :
OpenAIRE
Journal :
Medicinal Chemistry Research
Accession number :
edsair.doi...........58efbb0df2956ac2a39ae83998da07ab