共查询到20条相似文献,搜索用时 11 毫秒
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Shaa Zhou Sha Zhou Xuewen Hua Wei Wei Yongtao Xie Minggui Chen Xiangde Meng Ming Liu Lixia Xiong Na Yang Baolei Wang Zhengming Li 《中国化学》2016,34(12):1218-1224
Two series of N‐pyridylpyrazolecarboxamide derivatives were designed and synthesized by introducing D‐alanine acid esters and D‐serine acid esters into the skelecton of chlorantraniliprole. The obtained structures were characterized by 1H NMR, 13C NMR, elemental analysis and specific optical rotation analysis. Preliminary bioassays indicated that some compounds displayed excellent insecticidal activities against Mythimna separate and Plutella xylostella in comparison with chlorantraniliprole. In particular, IIq showed excellent insecticidal activity against Plutella xylostella with a mortality rate of 90% at 0.01 mg·L?1. A 3D‐QSAR (CoMSIA) study was performed in order to disclose the insecticidal structure‐activity relationship and indicate the future work. The CoMSIA study demonstrated that large substitutes and electron deficient groups at the 3‐position of pyrazole ring are favorable, the same as a small group near the ester groups of amino acid. 相似文献
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Sha Zhou Tao Yan Sha Zhou Xuewen Hua Baolei Wang Yucheng Gu Lixia Xiong Yongqiang Li Zhengming Li 《中国化学》2014,32(7):567-572
Due to a novel mode action, low toxicity to mammals and low residue characteristics, phthalic acid diamides have aroused considerable interests in agricultural chemistry. With introduction of N‐cyano, N‐trifluoroacetyl, N‐carbamoylsulfiliminyl and sulfoximinyl substituents into phthalamides, 12 novel derivatives containing trifluoromethyl moiety were designed and synthesized. All title compounds were characterized by 1H NMR and high‐resolution mass spectrometry. The preliminary results of biological activity assessment indicated that some title compounds exhibited moderate to good insecticidal activities against oriental armyworm (Pseudaletia separata Walker). In particular, Va gave higher activity against oriental armyworm and diamondback moth. The present work reported that the new trifluoromethylated diamides incorporating N‐trifluoroacetylsulfoximinyl moieties are potential lead compounds for further structure optimization, providing some insight into the relating structure‐activity relationship. 相似文献
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A series of novel phthalic diamide derivatives containing 1,2,3‐triazole moiety were synthesized using one‐pot click chemistry approach and characterized by 1H NMR and HRMS. The insecticidal activity against armyworm (Mythimna separata), Tetranychu scinnabarinus and cowpea aphid (Aphis craccivora) was evaluated. Compounds 4II‐a and 4II‐i showed 50% insecticidal activity against armyworm (Mythimna separata) at the concentration of 4 mg/L and one‐third of the compounds had moderate activity against Tetranychus cinnabarinus at 500 mg/L. 相似文献
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Two series of novel anthranilic diamide insecticide containing trifluoroethyl ether were designed and synthesized, and their structures were characterized by 1H NMR spectroscopy, elemental analysis and single crystal X‐ray diffraction analysis. The insecticidal activities of the new compounds were evaluated. The results of bioassays indicated that some of these title compounds exhibited excellent insecticidal activities. The insecticidal activities of compounds 19a , 19b , 19d , 19g , 19k and 19m against oriental armyworm at 2.5 mg·kg?1 were 100%. The larvicidal activities of 19a , 19b , 19c , 19d , 19e , 19g and 19n against diamond‐back moth were 100% at 0.1 mg·kg?1. Surprisingly, most of them still exhibited perfect insecticidal activity against diamond‐back moth when the concentration was reduced to 0.05 mg·kg?1, which was higher than the commercialized Chlorantraniliprole. 相似文献
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Huangong Li Yangyang Zhao Pengwei Sun Li Gao Yuxin Li Lixia Xiong Na Yang Sha Zhou Zhengming Li 《中国化学》2021,39(1):75-80
To search for potent insecticides targeting at ryanodine receptors (RyRs), a series of novel anthranilic diamides analogs containing 4‐chlorine N‐pyridylpyrazole were designed and synthesized. Their insecticidal activities were evaluated and the preliminary structure‐activity relationships (SARs) were discussed. The insecticidal results showed that some of the compounds (8a—8h, 8m, 8n) exhibited good larvicidal activities against oriental armyworm at 2.5 mg·L–1, and compound 8m possessed 60% insecticidal activity at 0.5 mg·L–1. For diamondback moth, 8m exhibited better activity than Chlorantraniliprole at a hundred fold preference. The calcium imaging technique experiment results suggested that compound 8m could increase the intracellular [Ca2+]i. With the neurons preincubated experiment, the results confirmed that the target of this series of compounds could be RyRs in the central larvae neurons of oriental armyworm. The results indicated that compound 8m could respond as a potential modulator of the insect ryanodine receptor. 相似文献
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《中国化学》2018,36(2):129-133
The sulfoximine group has been evaluated as a pharmacophore. Introducing the sulfoximine structure into medicinal compounds as exciting motifs has brought opportunities in drug discovery. In order to develop new ryanodine receptor (RyR) modulators, a series of phthalamides containing sulfoximine derivatives were designed, synthesized, and evaluated against oriental armyworm and diamondback moth for their insecticidal activities. These studies helped to elucidate the electronic and structural requirements around the sulfoximine motif for insecticidal activity. All new structures were synthesized and characterized by 1H NMR, 13C NMR, HRMS and bioassay and a preliminary structure − activity relationship (SAR) was discussed. The biological assessment indicated that most title compounds showed good to excellent larvicidal activities. Compounds Ia , Ie , and If gave excellent insecticidal activity against oriental armyworm, which showed 100% larvicidal activity at 0.5 mg/L. All compounds showed 100% larvicidal activity at 0.1 mg/L against diamondback moth. In particular, the larvicidal activities of Ie , If , and Ih at 0.0001 mg/L were 50%, 20%, and 40%, respectively, reaching an activity as high as that of the commercial flubendiamide (40%, 0.0001 mg/L). Therefore, Ia , Ie , If and Ih could be considered as new lead structures for the development of new ryanodine receptor (RyR) modulators. 相似文献
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以昆虫乙酰胆碱受体为作用靶标的新烟碱类杀虫剂属于高效、高选择性和环境友好的杀虫剂,依据新烟碱类杀虫剂活性与结构关系,以吡虫啉及其类似物NTN32692为先导结构,在咪唑啉环位置并入可以增强分子脂溶性的六元环基团,设计合成了9个未见文献报道的硝基亚甲基类新烟碱化合物,所有目标化合物的结构均经1H NMR、IR和HR-MS测试技术的确证。初步的生物活性测试结果表明,在500 mg/L下所有目标化合物对豆蚜(Aphis craccivora)都有一定的杀死活性,其中活性最高的化合物4对豆蚜(Aphis craccivora)的校正死亡率为73.0%。并对目标化合物5a~5h的合成方法进行了探讨。 相似文献
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Vijaya Kabra Sunita Mitharwal Swaroop Singh 《Phosphorus, sulfur, and silicon and the related elements》2013,188(9):2431-2442
A new series of dithiophosphonates has been synthesized using cycloiminium halides of pyridine, thiazole, and benzothiazole as starting material, dichlorophenylphosphine as phosphorylating agent, and 2-propanethiol as nucleophilic substituent. These compounds were tested for their insecticidal activity against a polyphagous insect plutella xylostella and found to exhibit potent pesticidal activity. 相似文献
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为了寻找具有较好生物活性的吡唑肟醚类衍生物,基于唑螨酯的结构,在吡唑环的4-位引入1,3,4-噁二唑结构,设计合成了15个结构新颖的吡唑肟醚类化合物,它们的结构通过1H NMR、13C NMR、元素分析等手段得到表征.生测研究表明,部分目标化合物在500和100μg/mL浓度下对粘虫(Oriental armyworm)或蚜虫(Aphis medicaginis)都有较好的杀虫效果,其中10a, 10e, 10f和10j在100μg/mL时对粘虫有100%的杀死率, 10g, 10j和10l在100μg/mL时对蚜虫有100%的杀虫活性.另外, 10l在500μg/mL浓度下对朱砂叶螨(Tetranychus cinnabarinus)也具有100%的杀灭效果. 相似文献
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Ten novel neonicotinoid derivatives containing N‐oxalyl groups were designed and synthesized, and their structures were characterized by 1H NMR, MS, IR, elemental analysis and single crystal X‐ray diffraction analysis. The insecticidal activities of the new compounds were evaluated. The results of bioassays indicated that some of these title compounds exhibited excellent insecticidal activities. 相似文献
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Xingan Cheng Huiqing He Fangyun Dong Chunbao Charles Xu Hanhui Zhang Zhanmei Liu Xiaojing Lv Yuehua Wu Xuhong Jiang Xiangjing Qin 《Molecules (Basel, Switzerland)》2022,27(15)
Matrine is a traditional botanical pesticide with a broad-spectrum biological activity that is widely applied in agriculture. Halopyrazole groups are successfully introduced to the C13 of matrine to synthesize eight new derivatives with a yield of 78–87%. The insecticidal activity results show that the introduction of halopyrazole groups can significantly improve the insecticidal activity of matrine on Plutella xylostella, Mythimna separata and Spodoptera frugiperda with a corrected mortality rate of 100%, which is 25–65% higher than matrine. The fungicidal activity results indicate that derivatives have a high inhibitory effect on Ceratobasidium cornigerum, Cibberella sanbinetti, Gibberrlla zeae and Collectot tichum gloeosporioides. Thereinto, 4-Cl-Pyr-Mat has the best result, with an inhibition rate of 23–33% higher than that of matrine. Therefore, the introduction of halogenated pyrazole groups can improve the agricultural activity of matrine. 相似文献
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含1,2,3-噻二唑的邻甲酰胺基苯甲酰胺类化合物的合成、晶体结构与生物活性 总被引:7,自引:0,他引:7
以取代邻氨基苯甲酸为起始原料, 设计并合成了一系列未见文献报道的含1,2,3-噻二唑的邻甲酰胺基苯甲酰胺类化合物. 所有化合物的结构均经元素分析和1H NMR确证, 并且采用X射线单晶衍射分析方法测定了化合物7g的结构. 初步的生物活性试验结果表明, 部分化合物具有一定的杀菌活性. 相似文献
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本文合成了8个未见文献报道的类似于氯虫苯甲酰胺的化合物——含硫氰基邻甲酰氨基苯甲酰胺类化合物,并用核磁共振氢谱、碳谱以及高分辨质谱予以表征。并且对这8个化合物针对小菜蛾和斜纹夜蛾的毒力进行测试并与氯虫苯甲酰胺进行对比,发现这8个化合物均对小菜蛾和斜纹夜蛾都具有较好的杀灭活性,尽管其活性比氯虫苯甲酰胺稍弱,但也非常接近,可以作为候选农药进行进一步考察。 相似文献
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以1-溴甲基-2-(4-氯苯基)-3-氰基-4-溴-5-三氟甲基吡咯为起始原料合成了3个新颖的N-桥连芳基吡咯类衍生物5a~5c. 通过氢谱、红外、元素分析及X射线单晶衍射确证了结构. 发现当2-(4-氯苯基)-3-氰基-4-溴-5-三氟甲基吡咯分别与S2Cl2, SCl2, 次磺酰氯, 亚磺酰氯反应时, 均未得到预期的N桥连产物, 却得到了Br被S取代的非预期产物. 杀虫杀螨活性结果显示目标产物5a~5c对东方粘虫、尖音库蚊幼虫、朱砂叶螨具有选择性, 如5a对东方粘虫具有很好的杀虫活性, 5a和5b在0.5 mg8226;g-1浓度下对尖音库蚊的杀虫活性为100%, 5b对朱砂叶螨具有很好的杀螨活性, 达到了商品化品种溴虫氰的水平. 相似文献
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设计,合成了8个新的含N-吡啶基吡唑杂环的邻氨基苯甲酸酯类化合物,结构经FTIR, MS, 1H NMR 和元素分析确证,并且采用X-射线衍射分析方法确证了具有较好生物活性的化合物14d的结构。并且对这些化合物进行了杀虫活性测试,结果表明目标化合物在200 µg·mL-1对粘虫 (Mythimna separata Walker)具有一定的杀虫活性,其中14d,14f,14h在1 µg·mL-1对淡色库蚊(Culex pipiens pallens)具有很好的杀幼虫活性。 相似文献
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A series of novel N‐pyridylpyrazole carbonyl thioureas were designed and synthesized. Their structures were characterized by melting points, 1H NMR, IR and elemental analysis or HRMS. The bioassay tests indicated that some of these compounds exhibited moderate insecticidal activity against Mythimna separata Walker and Culex pipiens pallens. Among 17 compounds, 5n and 5p showed 100% larvicidal activity against Mythimna separata Walker at the test concentration of 100 mg/L. 相似文献
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Changchun Wu Yuxin Li Ming Liu Jingbo Liu Xuewen Hua Dongkai Zhang Lixia Xiong Na Yang Baolei Wang Zhengming Li 《中国化学》2016,34(11):1121-1128
In order to search for potent and environmental friendly insecticides with new modes of action, a series of pyranoside derivatives mimicking D‐myo‐inositol 1,4,5‐trisphosphate (IP3) were designed and synthesized according to the bioisosteric approach. The biological assay indicated that most of the new compounds showed moderate to good insecticidal activities against oriental armyworm (Mythimna separata) and diamondback moth (Plutella xylostella). Especially, compound 5g displayed 80% larvicidal activity against oriental armyworm at 50 mg/L. Meanwhile, 5a showed 100% and 70% larvicidal activities against diamondback moth at 50 and 25 mg/L, respectively. To further explore the mode of action, calcium imaging technique was applied to study the effects of 5a , 5g , and 5i on the intracellular calcium ion concentration ([Ca2+]i) in central neurons isolated from Spodoptera exigua. The results indicated that the tested compounds released stored calcium ions from endoplasmic reticulum. 相似文献