Acta Chimica Sinica ›› 2012, Vol. 70 ›› Issue (02): 151-160.DOI: 10.6023/A1105302 Previous Articles     Next Articles

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李英俊a, 李春燕a, 靳焜b, 孙淑琴a, 周晓霞a   

  1. a 辽宁师范大学化学化工学院 大连 116029;
    b 大连理工大学精细化工国家重点实验室 大连 116012
  • 投稿日期:2011-05-30 修回日期:2011-07-25 发布日期:2012-02-25
  • 通讯作者: 李英俊
  • 基金资助:


Synthesis and Biological Activities of Novel Benzoxazolinone/Benzothiazolone Derivatives Containing Oxadiazole Moiety

Li Yingjuna, Li Chunyana, Jin Kunb, Sun Shuqina, Zhou Xiaoxiaa   

  1. a College of Chemistry and Chemical Engineering, Liaoning Normal University, Dalian 116029;
    b State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116012
  • Received:2011-05-30 Revised:2011-07-25 Published:2012-02-25
  • Supported by:

    Project supported by the Natural Science Foundation of Liaoning Province (No.20102126).

Thirty novel benzoxazolinone/benzothiazolone derivatives (6) containing oxadiazole moiety were synthesized by 2-aminophenol or 2-minothiophenol and urea as starting materials via a series of reactions. The structures of new intermediate 4 and the target compounds 6 were characterized by IR, 1H NMR spectra and elemental analysis. The synthesized target compounds were screened for the anticancer, antiinflammatory and immunoregulatory activities. The results indicated that some compounds exhibited weak activities in the anticancer and immunoregulatory fields, while all of them were found to be inactive against TNF-α and Cdc25B phosphatase.

Key words: benzoxazolinone/benzothiazolone, oxadiazole, synthesis, characterization, bioactivity