有机化学 ›› 2020, Vol. 40 ›› Issue (3): 782-786.DOI: 10.6023/cjoc201909023 上一篇    下一篇

研究简报

双酰胺类化合物的合成及生物活性研究

杨森, 邹文倩, 陶敏, 马天扬, 刘幸海, 翁建全, 谭成侠   

  1. 浙江工业大学化学工程学院 杭州 310014
  • 收稿日期:2019-09-16 修回日期:2019-10-18 发布日期:2019-11-07
  • 通讯作者: 谭成侠 E-mail:tanchengxia@zjut.edu.cn
  • 基金资助:
    国家重点研发计划(No.2017YFD0200507)资助项目.

Synthesis and Biological Activity of Diamide Compounds

Yang Sen, Zou Wenqian, Tao Min, Ma Tianyang, Liu Xinghai, Weng Jianquan, Tan Chengxia   

  1. College of Chemical Engineering, Zhejiang University of Technology, Hangzhou 310014
  • Received:2019-09-16 Revised:2019-10-18 Published:2019-11-07
  • Supported by:
    Project supported by the National Key R&D Program (No. 2017YFD0200507).

为了寻找高活性农药先导化合物,以甲霜灵为先导,通过活性基团拼接原理,设计合成了一系列未见文献报道的双酰胺类化合物,其结构经1H NMR、13C NMR和HRMS表征.初步的生物活性测试结果表明:在50 mg/L测试浓度下,化合物5j对黄瓜霜霉病显示出85%的抑制率;在500 mg/L剂量下,多数目标化合物对粘虫表现出较好的杀虫活性,其中化合物5b5f5g5h5i5l对粘虫的致死率高达100%,在250 mg/L测试浓度下,化合物5f5h5l对粘虫的致死率为50%.

关键词: 双酰胺类化合物, 合成, 生物活性

In order to find pesticidal lead compounds with high activity, a series of novel diamide compounds were designed and synthesized by using metalaxyl as a leading compound, as well as the principle of active substructure combination. The structures of the target compounds were confirmed by 1H NMR, 13C NMR and HRMS. The preliminary bioassay showed that compound 5j showed an 85% inhibition rate against Pseudoperoniospora cubensis at 50 mg/L, most of the target compounds had good insecticidal activity against Oriental armyworm at 500 mg/L, and compounds 5b, 5f, 5g, 5h, 5i and 5l have a mortality rate of 100% against Oriental armyworm. At 250 mg/L, the mortality rate of compounds 5f, 5h and 5l against Oriental armyworm was 50%.

Key words: diamide compound, synthesize, biological activity