Synthesis and antibacterial activity of novel chalcone derivatives bearing a coumarin moiety

  • Yi-Hui Wang
  • Shi-Chun Jiang
  • Ying Chen
  • Tao Guo
  • Rong-Jiao Xia
  • Xu Tang
  • Ming HeEmail author
  • Wei XueEmail author
Original Paper


A series of novel chalcone derivatives, that bear a coumarin moiety, were designed and synthesized, and their structures were confirmed via 1H NMR, 13C NMR, and H RMS. The bioassay results indicated that most title compounds exhibited remarkable antibacterial effects. Notably, compound 3a presented the most efficient antibacterial activity against Xanthomonas oryzae pv. Oryzae (Xoo), with median effect concentration (EC50) value of 49.77 μg/mL, which was far preferable than that of thiodiazolecopper (179.93 μg/mL). Meanwhile, compound 3n was identified as the best potential antibacterial agent against Xanthomonas axonopodis pv. citri (Xac), with EC50 value of 48.04 μg/mL, which far surpassed that of thiodiazolecopper (162.48 μg/mL). Furthermore, compound 3i indicated excellent antibacterial activity against Ralstonia solanacearum (Rs), with EC50 value of 65.04 μg/mL, which was far superior to that of thiodiazolecopper (126.89 μg/mL). This study indicated that chalcone hybrids, bearing a coumarin moiety, are worthy of further investigation as potential antibacterial drugs.


Synthesis Chalcone Coumarin Antibacterial activity 



The authors gratefully acknowledge the financial support of the National Key Research and Development Program of China (no. 2017YFD0200506), the National Nature Science Foundation of China (nos. 21867003, 21462012).

Supplementary material

11696_2019_802_MOESM1_ESM.doc (2.5 mb)
Supplementary material 1 (DOC 2609 kb)


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Copyright information

© Institute of Chemistry, Slovak Academy of Sciences 2019

Authors and Affiliations

  1. 1.State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of EducationGuizhou UniversityGuiyangChina

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