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有机化学
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有机化学 ›› 2010, Vol. 30 ›› Issue (9): 1366-1371. 上一篇    下一篇

研究论文

Nε-苯胺酰基-Nα-(3-取代苯基异噁唑-5-基羰基)赖氨酸类化合物的合成及其除草活性研究

胡德金，刘素芳，黄统辉，涂海洋*，李伟国，朱晓磊，张爱东   

  1. (华中师范大学化学学院 农药与化学生物学教育部重点实验室 武汉 4300791)
  • 收稿日期:2009-01-05 修回日期:2010-05-04 发布日期:2010-04-30
  • 通讯作者: 张爱东 E-mail:adzhang@mail.ccnu.edu.cn
  • 基金资助:

    国家973计划前期研究专项( No. 2007CB116302);国家级.国家自然科学基金

Synthesis and Herbicidal Activities of Nε-Anilinocarbonyl-Nα-{3-[(un)- substituted phenyl]isoxazol-5-ylcarbonyl}lysine Derivatives

HU De-Jin, LIU Su-Fang, HUANG Tong-Hui, TU Hai-Yang, LI Wei-Guo, ZHU Xiao-Lei, ZHANG Ai-Dong   

  1. (Key Laboratory of Pesticide and Chemical Biology of Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079)
  • Received:2009-01-05 Revised:2010-05-04 Published:2010-04-30
  • Contact: Aidong ZHANG E-mail:adzhang@mail.ccnu.edu.cn

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植物细胞内囊体中的D1蛋白酶是近年来发现的潜在的除草剂作用靶标. 以异噁唑甲酰赖氨酸脲先导结构信息为基础, 设计合成了未见报道的异噁唑甲酰赖氨酸类化合物11个. 目标化合物分子结构经IR, 1H NMR, 元素分析予以确证. 平皿法活体生物活性测试表明部分化合物具有中等除草活性; 化合物8h的离体生物活性测试表明其对D1蛋白酶有一定的抑制作用.

关键词: D1蛋白酶, 抑制剂, 异噁唑酰赖氨酸, 合成, 除草剂

Recently the D1 protease locating in the thylakoids of higher plants was found to be a potential herbicidal target. Based on one lead hit Nα-(isoxazol-5-ylcarbonyl)lysine of D1 protease inhibi-tors, a series of novel Nε-anilinocarbonyl-Nα-{3-[(un)substituted phenyl]isoxazol-5-ylcarbonyl}lysine derivatives were designed and synthesized, and their molecular struc-tures were verified with IR, 1H NMR, and elemental analysis. The biological activity examined in vivo demonstrated that most of the compounds exhibited moderate herbicidal activities. Mean-while, the enzyme activity of one compound 8h was tested against the spinach D1 protease and the result showed its inhibitive effect against the enzyme.

Key words: D1 protease, inhibitor, isoxazolecarbonyllysine derivative, synthesis, herbicide