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Solid-phase Synthesis of [4.4] Spirocyclic Oximes
Published on: February 6, 2019
Synthesis, anti-oomycete activity, and SAR studies of paeonol derivatives
Yue-E Tian1, Di Sun1, Xiao-Xiao Han1
1Laboratory of Pharmaceutical Design and Synthesis, Department of Plant Protection, College of Forestry, Henan University of Science and Technology, Luoyang 471023, China.
Abstract:
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].
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