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

doi:10.6023/A1105302

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

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新型含噁二唑环的苯并噁/噻唑啉酮衍生物的合成、表征及生物活性

李英俊^a, 李春燕^a, 靳焜^b, 孙淑琴^a, 周晓霞^a

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 E-mail:chemlab.lnnu@163.com
基金资助:
辽宁省自然科学基金(No.20102126)资助项目.

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

Li Yingjun^a, Li Chunyan^a, Jin Kun^b, Sun Shuqin^a, Zhou Xiaoxia^a

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

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Li Yingjun, Li Chunyan, Jin Kun, Sun Shuqin, Zhou Xiaoxia. Synthesis and Biological Activities of Novel Benzoxazolinone/Benzothiazolone Derivatives Containing Oxadiazole Moiety[J]. Acta Chimica Sinica, 2012, 70(02): 151-160.

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新型含噁二唑环的苯并噁/噻唑啉酮衍生物的合成、表征及生物活性

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

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