4.7 Article

Design, Synthesis, and Biological Evaluation of Novel 1,4-Pentadien3-one Derivatives Containing a Sulfonamide Moiety

Journal

JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
Volume 70, Issue 51, Pages 16096-16105

Publisher

AMER CHEMICAL SOC

Keywords

1,4-pentadien-3-one; sulfonamide moiety; antifungal; antibacterial; antiviral

Funding

  1. National Natural Science Foundation of China [32072446]
  2. Science Foundation of Guizhou Province [20192452]
  3. Natural Science Research Project of Guizhou Education Department [2018009]
  4. Science and Technology Program of Guizhou Province [20191139]
  5. Young Science and Technology Talents Development Program of Education Department of Guizhou Province [2018251]

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Novel 1,4-pentadien-3-one derivatives with a sulfonamide moiety were synthesized and their activities against fungi, bacteria, and viruses were tested. These compounds exhibited potent antibacterial and antifungal effects, and some showed promising antiviral activity. The study suggests that active splicing can enhance the biological activity of natural compounds, providing potential for the development of novel pesticides.
Novel 1,4-pentadien-3-one derivatives containing a sulfonamide moiety were synthesized, and their antifungal, antibacterial, and antiviral activities were verified. These compounds exhibited better activity against five bacteria, with EC50 values ranging from 9.6 to 60.1 mu g/mL, prominently, which are superior to those of the commercial agent. A great amount of compounds had excellent fungicidal activity in vitro at 100 mu g/mL. Strikingly, compound E6 exhibited moderate activity against Phytophthora litchii than azoxystrobin, with the EC50 value of compound E6 (0.5 mu g/mL) drawing near azoxystrobin (0.3 mu g/mL). Furthermore, compound E17 had a marked impact on in vivo anti-tobacco mosaic virus, according to the data of microscale thermophoresis, with a Kd value of the intermolecular binding force of 0.002 +/- 0.001 mu M, which was better than the commercial agent of ningnanmycin (Kd = 0.121 +/- 0.031 mu M). In addition, the results of these studies suggest that the use of active splicing can improve the biological activity of natural compounds and provide further complement to the development of novel pesticides.

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