有机化学 ›› 2013, Vol. 33 ›› Issue (05): 1069-1073.DOI: 10.6023/cjoc201211048 上一篇    下一篇

研究论文

环状多聚硫醚化合物的合成及生物活性研究

陈静, 姚励功, 郭跃伟, 龚景旭   

  1. 中国科学院上海药物研究所 新药研究国家重点实验室 上海 201203
  • 收稿日期:2012-11-28 修回日期:2012-12-28 出版日期:2013-05-25 发布日期:2013-01-07
  • 通讯作者: 龚景旭,jxgong@mail.shcnc.ac.cn;Tel.:021-50805813. E-mail:jxgong@mail.shcnc.ac.cn;Tel.:021-50805813.
  • 基金资助:

    国家自然科学基金(Nos. 81072572, 81273430, 21021063, 40976048, 31070310)、国家海洋“863”计划(Nos. 2011AA09070102, 2013AA092902)、新药研究国家重点实验室项目(Nos. SIMM1203ZZ-03, SIMM1105KF-04, SIMM1203KF-12)、欧盟第七框架协议部分(No. 246987)资助项目.

Synthesis and Bioactivity of Cyclic Polysulfides

Chen Jing, Yao Ligong, Guo Yuewei, Gong Jingxu   

  1. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203
  • Received:2012-11-28 Revised:2012-12-28 Online:2013-05-25 Published:2013-01-07
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 81072572, 81273430, 21021063, 40976048, 31070310), the National Marine “863” Project (Nos. 2011AA09070102, 2013AA092902), the State Key Laboratory of Drug Research/Shanghai Institute of Materia Medica Projects (Nos. SIMM1203ZZ-03, SIMM1105KF-04 and SIMM1203KF-12) and partially funded by the EU 7th Framework Programme-IRSES Project (No. 246987).

通过二硫醇化合物与二氯代物缩合, 再酰化的方法合成了14个具有环状结构的新颖多聚硫醚化合物, 其中12个为新化合物, 得到的化合物经1H NMR, 13C NMR和HREIMS确证其结构, 部分化合物还经晶体X衍射方法确证. 通过对II型糖尿病靶标蛋白酪氨酸磷酸酯酶(PTP1B)抑制活性的分析, 发现一些化合物具有一定的PTP1B抑制活性.

关键词: 环状多聚硫醚, 合成, PTP1B抑制活性

Fourteen cyclic polythiaethers, twelve of them are new compounds, were synthesized by condensation of dithiol with dichlorided compounds and then acylation. Their structures were characterized by 1H NMR, 13C NMR, HREIMS techniques. Some of the compounds were detected by X-ray. The PTP1B inhibitory activities of these compounds were tested.

Key words: cyclic polythioethers, synthesis, PTP1B inhibitory activities