Chinese Journal of Organic Chemistry ›› 2020, Vol. 40 ›› Issue (1): 108-114.DOI: 10.6023/cjoc201906014 Previous Articles     Next Articles


黎勇坤, 唐燕玲, 李敏欣, 杨小碧, 高慧, 毛泽伟   

  1. 云南中医药大学中药学院 昆明 650500
  • 收稿日期:2019-06-13 修回日期:2019-08-16 发布日期:2019-09-12
  • 通讯作者: 毛泽伟
  • 基金资助:

Synthesis and Antibacterial Activity of Thienyl Chalcone Derivatives Bearing Piperazine Moiety

Li Yongkun, Tang Yanling, Li Minxin, Yang Xiaobi, Gao Hui, Mao Zewei   

  1. College of Pharmaceutical Science, Yunnan University of Chinese Medicine, Kunming 650500
  • Received:2019-06-13 Revised:2019-08-16 Published:2019-09-12
  • Supported by:
    Project supported by the National Natural Science Foundation of China (No. 81560620) and the Yunnan Provincial Science and Technology Department-Applied Basic Research Joint Special Funds of Yunnan University of Chinese Medicine (No. 2017FF117(-023)).

Chalcone derivatives are a kind of 1,3-diphenylacrylketone compounds with a broad range of biological activities. A series of new thienyl chalcone derivatives bearing piperazine moiety have been designed and prepared based on the principle of bioisosteres and molecular hybridization. Their antibacterial activities against Staphylococcus aureus Rosenbach, Escherichia coli and Bacillus subtilis were evaluated. The results showed that thienyl chalcone derivatives exhibited good selective inhibitory activities against the three tested strains, respectively. Especially, (E)-1-[4-(4-methylcinnamatemethylpiperazinyl)-phenyl]-3-(thien-2-yl)propyl-2-ketene (4b) and (E)-1-{4-[4-(2-oxophenethyl)piperazinyl]phenyl}-3-(thien-2-yl)propyl-2-kete-ne (4e) were found to be very sensitive to Bacillus subtilis, and the minimum inhibitory concentration (MIC) is 4.0 μg/mL against Bacillus subtilis.

Key words: thiophene, chalcone, antibacterial activity, MIC