Chin. J. Org. Chem. ›› 2016, Vol. 36 ›› Issue (4): 818-825.DOI: 10.6023/cjoc201510005 Previous Articles     Next Articles

ARTICLE

含1,2,4-三唑席夫碱的新型喹唑啉-2,4-二酮类衍生物的合成及其抗细菌活性研究

潘顶伍, 杜欢, 吕新阳, 鲍小平   

  1. 贵州大学精细化工研究开发中心 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农业生物工程重点实验室 贵阳 550025
  • 收稿日期:2015-10-09 修回日期:2015-11-05 发布日期:2015-12-10
  • 通讯作者: 鲍小平 E-mail:baoxp_1980@aliyun.com
  • 基金资助:

    国家自然科学基金(No.21362003)资助项目.

Synthesis and Antibacterial Activities of Novel Quinazoline-2,4-dione Derivatives Containing the 1,2,4-Triazole Schiff-Base Unit

Pan Dingwu, Du Huan, Lü Xinyang, Bao Xiaoping   

  1. State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025
  • Received:2015-10-09 Revised:2015-11-05 Published:2015-12-10
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 21362003).

Eighteen novel quinazoline-2,4-dione derivatives containing the 1,2,4-triazole Schiff-base unit were designed and synthesized, based on the connection method of active fragments. Their structures were characterized by 1H NMR, 13C NMR, MS, IR and elemental analysis. The preliminary antibacterial test indicated that all the target compounds possessed an excellent inhibition activity (≥ 93%) against Xanthomonas oryzae pv. oryzae (Xoo) at the concentration of 200 μg/mL, which was obviously better than those of control agents thiodiazole-copper and bismerthiazol. Compounds 7a, 7c~7g and 7j~7l still displayed 100% inhibition rate against Xoo even at the concentration of 100 μg/mL. Moreover, all the target compounds exhibited a certain inhibition activity against Xanthomonas axonopodis pv. citri, but no inhibition activity against Ralstonia solanacearum.

Key words: 1,2,4-triazole Schiff-base, quinazoline-2,4-dione, synthesis, antibacterial activity