熊果酸酯衍生物的半合成、抗卵菌和抗真菌活性
Semisynthesis, anti-oomycete and anti-fungal activities of ursolic acid ester derivatives.
作者信息
Zhu Lina, Tian Yuee, Wang Tiewei, Huang Xiaobo, Zhou Lin, Shengming Liu, Chen Genqiang, Che Zhiping
机构信息
Laboratory of Pesticidal Design & Synthesis, Department of Plant Protection, College of Horticultrue and Plant Protection, Henan University of Science and Technology, Luoyang, China.
ShanDong New Power Biology Science &Technology Co., Ltd, Jinan, China.
出版信息
Nat Prod Res. 2024 Mar;38(6):906-915. doi: 10.1080/14786419.2023.2207135. Epub 2023 Apr 28.
Using ursolic acid (UA) as the lead compound, thirteen UA ester derivatives ( and -) were synthesized by modifying their C-3 and C-28 positions, respectively, and their structures were well characterized by H NMR, C NMR, HRMS and melting points. Furthermore, we evaluated the anti-oomycete and anti-fungal activities of these compounds against and . The results showed that compound exhibited prominent anti-oomycete and anti-fungal activities, and the median effective concentration (EC) values of against and were 70.49 and 113.21 mg/L, respectively. This study suggested that the anti-oomycete and anti-fungal activities of esters synthesized by introducing acyloxy group at C-3 position of UA was more conspicuous than that of esters synthesized by introducing benzyloxy group at C-28 position. This result will pave the way for further modification of UA to develop potential new fungicides.
以熊果酸（UA）为先导化合物，分别通过修饰其C-3和C-28位合成了13种UA酯衍生物（ 和 -），并通过1H NMR、13C NMR、HRMS和熔点对其结构进行了充分表征。此外，我们评估了这些化合物对 和 的抗卵菌和抗真菌活性。结果表明，化合物 表现出显著的抗卵菌和抗真菌活性，其对 和 的半数有效浓度（EC）值分别为70.49和113.21 mg/L。该研究表明，在UA的C-3位引入酰氧基合成的酯的抗卵菌和抗真菌活性比在C-28位引入苄氧基合成的酯更显著。这一结果将为进一步修饰UA以开发潜在的新型杀菌剂铺平道路。
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