文献类型：期刊文献

英文题名：Antifungal Activity of Novel Isoindoline-2-Yl Putrescines as Potential Autophagy-Activated Fungicide

作者：Zhu, Lisong[1];Huang, Fengcheng[1];Wang, Hongye[1];Zhao, Yanjun[1];Luan, Shaorong[2];Xiao, Ciying[3];Huang, Qingchun[1]

机构：[1]East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Sch Chem & Mol Engn, Shanghai 200237, Peoples R China;[3]East China Univ Sci & Technol, Sch Biochem Engn, Shanghai 20037, Peoples R China

年份：2025

卷号：22

期号：2

外文期刊名：CHEMISTRY & BIODIVERSITY

收录：;WOS:【SCI-EXPANDED(收录号:WOS:001356904200001)】；

基金：This work was supported in part by the projects of Shanghai Science and Technology Plan in China (22 N41900100) and the National Natural Science Foundation of China (32372588).

语种：英文

外文关键词：Isoindoline-2-yl putrescine; In vivo antifungal activity; Molecular docking; Plant fungal pathogen

摘要：The exacerbation of plant fungal diseases necessitates the development of new fungicides to prevent outbreaks. In this study, five novel isoindoline-2-yl putrescines (ISPs) were synthesized, and their synthetic procedures and gram-scale preparation were explored. When tested at 50 mu g mL-1, ISPs did not significantly inhibit mycelial growth on agar plates. However, at 100 mu g mL-1, they demonstrated remarkable in vivo efficacy in mitigating Botrytis cinerea infection, especially ISP3 showed curative and protective activities of 91.9 % and 92.6 %, respectively. Moreover, ISP3 also effectively halted lesion expansion of gray mold, Sclerotic rot, and Fusarium scabs, while inducing excessive malformed top mycelial branches of B. cinerea and Sclerotinia sclerotiorum, suppressing sclerotia formation in S. sclerotiorum, and triggering autophagic vacuolization with numerous autophagosomes in the mycelia of these fungi. Molecular docking revealed that ISP3 effectively bound to the active site of BcAtg3, forming hydrogen bonds with Ser279, Gly343, Asp370, and Asp13, along with establishing a stable salt bridge with Asp13. Furthermore, ISP3 possessed favorable ADMET properties. These findings highlight ISP3 as a promising antifungal candidate through autophagy activation.