α-羟基-γ-丁内酯类衍生物的设计、合成及抗植物病毒活性  

Design,synthesis and anti-plant viral activity ofα-hydroxy-γ-butyrolactone derivatives

作　　者：贺宏伟 徐丹 徐功 HE Hongwei;XU Dan;XU Gong(Key Laboratory of Plant Protection Resources and Pest Management of Ministry of Education,College of Plant Protection,Northwest A&F University,Yangling 712100,Shaanxi Province,China;Shaanxi Key Laboratory of Natural Products&Chemical Biology,College of Chemistry&Pharmacy,Northwest A&F University,Yangling 712100,Shaanxi Province,China)

机构地区：[1]植保资源与病虫害治理教育部重点实验室,西北农林科技大学植物保护学院,陕西杨凌712100 [2]陕西省天然产物化学生物学重点实验室,西北农林科技大学化学与药学院,陕西杨凌712100

出　　处：《农药学学报》2023年第6期1261-1269,共9页Chinese Journal of Pesticide Science

基　　金：国家自然科学基金面上项目(22377099);中央高校基本科研业务费专项资金项目(2452019189,2452018318)。

摘　　要：为寻找具有高活性抗病毒化合物,开发绿色抗植物病毒剂,设计合成了21个α-羟基-γ-丁内酯类化合物,其结构经过核磁共振氢谱、碳谱以及高分辨质谱确认,并初步测定了它们对烟草花叶病毒(TMV)的钝化活性、保护活性和治疗活性。结果表明:该类化合物具有较好的抗TMV活性,其中化合物8o表现出显著的钝化活性,其EC_(50)值为226.2μg/mL,优于对照药剂病毒唑(EC_(50)值308.4μg/mL)。To identify highly effective antiviral compounds and develop green antiviral agents for plants,21α-hydroxy-γ-butyrolactone derivatives were designed and synthesized.Their structures were characterized using ^(1)H NMR,^(13)C NMR and HRMS.The in vivo antiviral activities against tobacco mosaic virus(TMV)were evaluated in three modes(inactivation,curative,and protective).Bioassay results revealed that many of the target compounds exhibited potent anti-TMV activities.Notably,compound 8o displayed prominent inactivation activity with an EC_(50) value of 226.2μg/mL,which was significantly superior to ribavirin(EC_(50)=308.4μg/mL).

关 键 词：天然产物 Γ-丁内酯 合成 抗植物病毒活性 烟草花叶病毒 

分 类 号：O626.2[理学—有机化学] TQ450.11[理学—化学]