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Natural product‐based fungicides discovery (II): Semisynthesis and biological activity of sarisan attached 3‐phenylisoxazolines as antifungal agents
Chemistry & Biodiversity ( IF 2.9 ) Pub Date : 2020-11-19 , DOI: 10.1002/cbdv.202000763
Zhiyan Liu 1, 2 , Jiangping Cao 1 , Xiaoting Yan 2 , Wanqing Cheng 2 , Xiaoguang Wang 2 , Ruige Yang 2 , Yong Guo 2
Affiliation  

Many phytopathogenic fungi cause severe damage to crop yields. In continuation of our research aimed at the discovery and development of natural products‐based fungicides, a series of thirty‐one sarisan attached 3‐phenylisoxazolines were synthesized and evaluated for their antifungal activities against five phytopathogenic fungi (B. cinerea, C. lagenarium, A. solani, F. solani, and F. graminearum). Among all title sarisan derivatives, compounds IV2, IV14 and IV23 showed potent antifungal activity against some phytopathogenic fungi. In particular, compound IV2 exhibited a broad‐spectrum and more potent antifungal activity against A. solani, F. solani, and F. graminearum than the commercial fungicide Hymexazol. In addition, compounds IV2, IV14 and IV23 also displayed relative low toxicity on normal NRK‐52E cells. This work will give some insights into the development of sarisan derivatives as new fungicide candidates in plant protection.

中文翻译:

基于天然产物的杀菌剂发现(II):作为抗真菌剂的 sarisan 附着的 3-苯基异恶唑啉的半合成和生物活性

许多植物病原真菌对作物产量造成严重损害。为了继续我们旨在发现和开发基于天然产物的杀菌剂的研究,合成了一系列 31 种附着有 3-苯基异恶唑啉的纱丽,并评估了它们对五种植物病原真菌(B. cinerea、C. lagenarium、 A. solani、F. solani 和 F. graminearum)。在所有标题 sarisan 衍生物中,化合物 IV2、IV14 和 IV23 对某些植物病原真菌显示出有效的抗真菌活性。特别是,化合物 IV2 表现出比商业杀菌剂 Hymexazol 更广谱和更有效的抗病曲霉、茄病镰刀菌和禾谷镰刀菌的抗真菌活性。此外,化合物IV2、IV14和IV23对正常NRK-52E细胞的毒性也相对较低。
更新日期:2020-11-19
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