Synthesis, Nematicidal Evaluation, and the Structure-Activity Relationship Study of Aurone Derivatives

被引:2
|
作者
Cao, Xiaofeng [1 ]
Wang, Mingxia [1 ]
Li, Zhong [1 ]
Xu, Xiaoyong [1 ]
机构
[1] East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China
基金
中国国家自然科学基金;
关键词
SHAFTS; scaffold hopping; nematicidal activity; aurone derivatives; SAR; INHIBITORY-ACTIVITY; HYBRID APPROACH; DISCOVERY; SHAFTS;
D O I
10.1021/acs.jafc.3c00627
中图分类号
S [农业科学];
学科分类号
09 ;
摘要
Plant-parasitic nematodes (PPNs) are one of the majorthreats tomodern agriculture. Chemical nematicides are still required for themanagement of PPNs. Based on our previous work, the structure of auroneanalogues was obtained using a hybrid 3D similarity calculation method(SHAFTS, SHApe-FeaTure Similarity). Thirty-seven compounds were synthesized.The nematicidal activity of target compounds against Meloidogyne incognita (root-knot nematode, M. incognita) was evaluated, and the structure-activityrelationship of synthesized compounds was analyzed. The results showedthat compound 6 and some of its derivatives exhibitedimpressive nematicidal activity. Among these compounds, compound 32 bearing 6-F showed the best in vitro and in vivo nematicidal activity. Its lethal concentration 50%after exposure to 72 h (LC50/72 h) value was 1.75mg/L, and the inhibition rate reached 97.93% in the sand at 40 mg/L.At the same time, compound 32 also exhibited excellentinhibition on egg hatching and moderate inhibition on the motilityof Caenorhabditis elegans (C. elegans).
引用
收藏
页码:8757 / 8768
页数:12
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