摘要
基于除草剂新靶标转酮醇酶,采用农药分子合理设计的方法,对化合物α-三联噻吩进行结构改造,以异噁唑胺为核心杂环,引入噻吩、呋喃、苯并咪唑等杂环结构,设计合成9个异噁唑胺类化合物5(a-i)。所有化合物均经1H NMR和元素分析验证,除草活性筛选发现,含有苯并咪唑基团的5c和5f表现出较高的除草活性,在200 mg/L浓度下,对马唐和反枝苋的根茎抑制率达到90%~96%,其优于阳性对照药剂丙炔氟草胺(80%~88%),表明以异噁唑胺为先导,引入苯并咪唑基团有利于提高化合物的除草活性,且5c和5f有潜力作为除草剂候选化合物,值得进一步结构优化。
Isoxazolamines 5(a-i)were designed and synthesized based on the target of transketolase.α-Terthiophene was chosen as the lead,and isoxazole was used as the core heterocyclic structure in the design,introduced by other heterocyclic structures such as thiophene,furan,and benzimidazole.Their structures were verified by 1H NMR and elemental analysis,and their herbicidal activities were screened,and showed that compounds 5c and 5f with benzimidazole groups as substructure displayed the highest herbicidal activity among them,and the inhibition rate were more than 90%against the tested weed root and stem,which was higher than the positive control Flumioxazin(88%).The results showed that benzimidazole group based on isoxazole as the core heterocyclic structure was beneficial to improve the herbicidal activity of the compounds,and 5c and 5f had the potential to be herbicide candidate compounds,which deserved for further optimization.
作者
王彦恩
刘晓凤
王红雨
高玉洁
张金林
WANG Yan’en;LIU Xiaofeng;WANG Hongyu;GAO Yujie;ZHANG Jinlin(College of Science,Hebei Agricultural University,Baoding 071001,China;College of Plant Protection,Hebei Agricultural University,Baoding 071001,China)
出处
《河北农业大学学报》
CAS
CSCD
北大核心
2021年第1期102-106,119,共6页
Journal of Hebei Agricultural University
基金
河北农业大学理工基金项目(LG201802)
河北省大学生创新创业训练计划资助项目(s202010086035)
国家自然科学基金资助项目(31871981)
河北省博士后科研项目择优资助(B2019005008).
关键词
杂草抗性
转酮醇酶
分子设计
异噁唑胺类
weed resistance
transketolase
molecular design
isoxazolamines
