Citation: Li Yongkun, Tang Yanling, Li Minxin, Yang Xiaobi, Gao Hui, Mao Zewei. Synthesis and Antibacterial Activity of Thienyl Chalcone Derivatives Bearing Piperazine Moiety[J]. Chinese Journal of Organic Chemistry, ;2020, 40(1): 108-114. doi: 10.6023/cjoc201906014 shu

Synthesis and Antibacterial Activity of Thienyl Chalcone Derivatives Bearing Piperazine Moiety

College of Pharmaceutical Science, Yunnan University of Chinese Medicine, Kunming 650500

Corresponding author: Mao Zewei, maozw@ynutcm.edu.cn
Received Date: 13 June 2019
Revised Date: 16 August 2019
Available Online: 13 January 2019
Fund Project: the Yunnan Provincial Science and Technology Department-Applied Basic Research Joint Special Funds of Yunnan University of Chinese Medicine 2017FF117(-023)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))the National Natural Science Foundation of China 81560620

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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.
- thiophene,
- chalcone,
- antibacterial activity,
- MIC
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