高等学校化学学报 ›› 2017, Vol. 38 ›› Issue (1): 35-40.doi: 10.7503/cjcu20160654

• 有机化学 • 上一篇    下一篇

酰胺类杨梅素衍生物的合成及抑菌活性

肖维, 阮祥辉, 李琴, 张菊平, 钟新敏, 谢艳, 王晓斌, 黄民国, 薛伟()   

  1. 绿色农药与农业生物工程国家重点实验室培育基地, 教育部绿色农药与生物工程重点实验室,贵州大学精细化工研究开发中心, 贵阳 550025
  • 收稿日期:2016-09-19 出版日期:2017-01-10 发布日期:2016-12-15
  • 作者简介:联系人简介: 薛 伟, 男, 博士, 教授, 主要从事新农药和新医药创制研究. E-mail: wxue@gzu.edu.cn
  • 基金资助:
    国家自然科学基金(批准号: 21462012)、 贵州省优秀青年科技人才项目(批准号: 201535)和贵州大学研究生创新基金(批准号: 2016078)资助.

Synthesis and Antibacterial Activities of Myricetin Derivatives ontaining Acidamide Moiety

XIAO Wei, RUAN Xianghui, LI Qin, ZHANG Juping, ZHONG Xinmin, XIE Yan, WANG Xiaobin, HUANG Minguo, XUE Wei*()   

  1. State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green esticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals,Guizhou University, Guiyang 550025, China
  • Received:2016-09-19 Online:2017-01-10 Published:2016-12-15
  • Contact: XUE Wei E-mail:wxue@gzu.edu.cn
  • Supported by:
    † Supported by the National Natural Science Foundation of China(No.21462012), the Excellent Young Talents of Science and Technology in Guizhou Province, China(No.201535) and the Innovation Fund for Graduate Student of Guizhou University, China(No.2016078).

摘要:

以杨梅素为先导化合物, 设计合成了12个酰胺类杨梅素衍生物; 利用核磁共振波谱(1H NMR和13C NMR)和高分辨质谱仪(HRMS)对其结构进行了确证. 初步抑菌活性测定结果表明, 该类化合物对水稻白叶枯病菌、 柑橘溃疡病菌和烟草青枯病菌均具有一定的抑制活性, 化合物3a, 3e, 3f, 3h和3k对3种植物病菌表现出较好的抑制活性, 其中200 μg/mL化合物3e对水稻白叶枯病菌和烟草青枯病菌的抑制活性均为100%, 超过对照药叶枯唑(抑菌活性分别为72.85%和75.86%).

关键词: 杨梅素衍生物, 酰胺, 抑菌活性

Abstract:

Twelve novel myricetin derivatives containing acidamide moiety were designed and synthesized from myricetin. All the compounds were characterized by 1H NMR, 13C NMR and HRMS. The preliminary bioassay results indicated that all of the title compounds exhibited a certain antibacterial activities in vitro against X. oryzae, X. citri and R. solanacearum. Moreover, These title compounds 3a, 3e, 3f, 3h and 3k displayed good antibacterial activities against the above three plant pathogenic bacteria. Especially, compound 3e displayed 100% inhibition rates against X. oryzae and R. solanacearum at 200 μg/mL, respectively, which is more than the control bismerthiazol(72.85% and 75.86%, repectively).

Key words: Myricetin derivatives, Acidamide, Antibacterial activity

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