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高等学校化学研究 ›› 2010, Vol. 26 ›› Issue (2): 225-229.

• Articles • 上一篇    下一篇

Synthesis and HIV-1 Integrase Inhibitory Activity of Furanone Derivatives

YU Sheng-hui, ZHAO Si-tai, LIU Chuan, ZHONG Yuan and ZHAO Gui-sen*   

  1. School of Pharmaceutical Sciences, Shandong University, Jinan 250012, P. R. China
  • 收稿日期:2009-04-21 修回日期:2009-07-13 出版日期:2010-03-25 发布日期:2010-05-25
  • 通讯作者: ZHAO Gui-sen. E-mail: guisenzhao@sdu.edu.cn
  • 基金资助:

    Supported by the National Natural Science Foundation of China(No.20872082) and the Natural Science Foundation of Shandong Province, China(No. Y2007C060).

Synthesis and HIV-1 Integrase Inhibitory Activity of Furanone Derivatives

YU Sheng-hui, ZHAO Si-tai, LIU Chuan, ZHONG Yuan and ZHAO Gui-sen*   

  1. School of Pharmaceutical Sciences, Shandong University, Jinan 250012, P. R. China
  • Received:2009-04-21 Revised:2009-07-13 Online:2010-03-25 Published:2010-05-25
  • Contact: ZHAO Gui-sen. E-mail: guisenzhao@sdu.edu.cn
  • Supported by:

    Supported by the National Natural Science Foundation of China(No.20872082) and the Natural Science Foundation of Shandong Province, China(No. Y2007C060).

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被引次数

4

摘要：

Twenty novel furanone derivatives, based on the structure of raltegravir which was the first HIV-1 integrase(IN) inhibitor approved by the United States Food and Drug Administration(US FDA), were designed, synthesized and characterized by 1H NMR, IR and MS. The biological activities of these compounds against HIV-1 IN in vitro were evaluated. The assay results indicate that the replacement of pyrimidinone with furanone decreased the inhibitory activity of the compounds to HIV-1 IN. Compounds 3i, 3j and 3t show moderate inhibitory activity against HIV-1 IN and selectively inhibit the strand transfer reaction.

关键词: HIV-1 integrase; Diketoacid; Furanone

Abstract:

Twenty novel furanone derivatives, based on the structure of raltegravir which was the first HIV-1 integrase(IN) inhibitor approved by the United States Food and Drug Administration(US FDA), were designed, synthesized and characterized by 1H NMR, IR and MS. The biological activities of these compounds against HIV-1 IN in vitro were evaluated. The assay results indicate that the replacement of pyrimidinone with furanone decreased the inhibitory activity of the compounds to HIV-1 IN. Compounds 3i, 3j and 3t show moderate inhibitory activity against HIV-1 IN and selectively inhibit the strand transfer reaction.

Key words: HIV-1 integrase; Diketoacid; Furanone