Synthesis, anti-oomycete activity, and SAR studies of paeonol derivatives.

Yue-E Tian, Di Sun, Xiao-Xiao Han, Jin-Ming Yang, Song Zhang, Nan-Nan Feng, Li-Na Zhu, Zhong-Yuan Xu, Zhi-Ping Che, Sheng-Ming Liu, Xiao-Min Lin, Jia Jiang, Gen-Qiang Chen

Journal of Asian natural products research 2021 Feb

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Three series of sulfonate derivatives of paeonol were synthesized and screened in vitro for their anti-oomycete activity against P. capsici, respectively. Among all the compounds, 4m displayed the best promising and pronounced anti-oomycete activity against P. capsici than zoxamide, with the EC50 values of 24.51 and 26.87 mg/L, respectively. The results show that acetyl and 4-OCH3 are two necessary groups. The existence of these two sites is closely related to the anti-oomycete activity. Relatively speaking, hydroxyl group is well tolerated, and the results showed that after modification of hydroxyl group with sulfonyl, the anti-oomycete activity was significantly increased. [Formula: see text].

Citation

Yue-E Tian, Di Sun, Xiao-Xiao Han, Jin-Ming Yang, Song Zhang, Nan-Nan Feng, Li-Na Zhu, Zhong-Yuan Xu, Zhi-Ping Che, Sheng-Ming Liu, Xiao-Min Lin, Jia Jiang, Gen-Qiang Chen. Synthesis, anti-oomycete activity, and SAR studies of paeonol derivatives. Journal of Asian natural products research. 2021 Feb;23(2):138-149