Synthesis and Nematicidal Activities of 1,2,3-Benzotriazin-4-one Derivatives against Meloidogyne incognita.
Synthesis and Nematicidal Activities of 1,2,3-Benzotriazin-4-one Derivatives against Meloidogyne incognita.
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DOI：
10.1021/acs.jafc.5b01762
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发表时间：
2015-08
影响因子：
6.1
通讯作者：
Gaolei Wang;Xiulei Chen;Yayun Deng;Zhong Li;Xiaoyong Xu
中科院分区：
文献类型：
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作者：
Gaolei Wang;Xiulei Chen;Yayun Deng;Zhong Li;Xiaoyong Xu
在碘化钾存在下，3-溴烷基-1，2，3-苯并三嗪-4-酮与2-氰基亚氨基-4-氧代噻唑烷钾盐反应，合成了一系列新的1，2，3-苯并三嗪-4-酮衍生物。活体杀线虫试验表明，部分化合物对黄瓜根结线虫病（Meloidogyne incognita）有较好的防治效果，在10.0 mg L（-1）浓度下，防治效果可达100%，表明1，2，3-苯并三嗪-4-酮衍生物可能是一种有潜力的新型杀线虫剂。杀线虫活性受分子中取代基类型、取代位置和接头长度的组合影响。并给出了具有较高抑制活性的化合物在5.0和1.0mg·L ~（-1）浓度下的抑制率数据。在体外试验中，没有一个化合物对M.无名氏正在研究体内和体外数据之间的显著差异。
A series of novel 1,2,3-benzotriazin-4-one derivatives were synthesized by the reaction of 3-bromoalkyl-1,2,3-benzotriazin-4-ones with potassium salt of 2-cyanoimino-4-oxothiazolidine in the presence of potassium iodide. Nematicidal assays in vivo showed that some of them exhibited good control efficacy against the cucumber root-knot nematode disease caused by Meloidogyne incognita, up to 100% at the concentration of 10.0 mg L(-1), which indicated that 1,2,3-benzotriazin-4-one derivatives might be potential for novel promising nematicides. The nematicidal activity was influenced by the combination of substituent type, substituted position, and linker length in the molecule. The inhibition rate data at the concentrations of 5.0 and 1.0 mg L(-1) for the compounds with high inhibitory activities were also provided. When tested in vitro, none of them showed direct inhibition against M. incognita. The investigation of a significant difference between in vivo and in vitro data is in progress.