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Synthesis of novel 4-thiazolidione derivatives as antibacterial agents against drug-resistant Staphylococcus epidermidis

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Abstract

A series of novel substituted 4-thiazolidione derivatives were designed, synthesized, and evaluated in vitro for their antibacterial activities, in comparison with methicillin and ampicillin. Compounds (7d, 7h–k) exhibit good potency in inhibiting the growth of Staphylococcus epidermidis (MIC: 1.57–3.13 μM). Further antibacterial effects of compounds (7d, 7h–k) were investigated using clinical isolates (methicillin-resistant Staphylococcus epidermidis and methicillin-resistant Staphylococcus aureus), in comparison with methicillin and levofloxacin. Compound 7k showed the most potent antibacterial activities among the synthesized compounds.

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Acknowledgments

We would like to thank Professor Guoqiang Lin, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, for his invaluable academic advice. This work was supported by the National Natural Science Foundation of China Grant no. 20942006 (S. Han), Grant no. 21072095 (S. Han), Grant no. 30800036 (D. Qu), Shanghai Municipal Committee of Science and Technology (08JC1401600), National High Technology Research and Development Program of China (863 Program 2011AA02A209) and Program for Changjiang Scholars and Innovative Research Team in University (Grant no. IRT1066).

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Authors and Affiliations

  1. College of Biotechnology and Pharmaceutical Engineering, Nanjing University of Technology, Nanjing, 210009, China

    Dan Zhao, Likang Zheng, Guozhen He & Shiqing Han

  2. Key Laboratory of Medical Molecular Virology of Ministry of Education and Ministry of Public Health, Institute of Medical Microbiology and Institutes of Biomedical Sciences, Shanghai Medical School of Fudan University, Shanghai, 200032, China

    Huayong Liu & Di Qu

Authors
  1. Dan Zhao
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  2. Huayong Liu
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  3. Likang Zheng
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  4. Guozhen He
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  5. Di Qu
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  6. Shiqing Han
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Corresponding authors

Correspondence to Di Qu or Shiqing Han.

Additional information

D. Zhao, H. Liu and L. Zheng contributed equally to this study.

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Zhao, D., Liu, H., Zheng, L. et al. Synthesis of novel 4-thiazolidione derivatives as antibacterial agents against drug-resistant Staphylococcus epidermidis . Med Chem Res 22, 3743–3750 (2013). https://doi.org/10.1007/s00044-012-0363-9

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  • DOI: https://doi.org/10.1007/s00044-012-0363-9

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