Synthesis and biological activities of novel 1,3,4-thiadiazole-containing pyrazole oxime derivatives

Synthesis and biological activities of novel 1,3,4-thiadiazole-containing pyrazole oxime derivatives
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新型1,3,4-噻二唑吡唑肟衍生物的合成及生物活性

DOI:
10.1016/j.bmcl.2016.04.094
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发表时间:
2016-08-01
影响因子:
2.7
通讯作者:
He, Haibing
He, Haibing
中科院分区:
医学4区
文献类型:
--
作者:
Dai, Hong;Li, Gang;He, Haibing

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设计并合成了一个新的含1,3,4-噻二唑基的吡唑肟文库。并对其杀螨杀虫活性进行了评价。生物活性测定结果表明,部分目标化合物具有良好的杀螨、杀虫性能。其中,化合物8m在50 mU g/m L浓度下对朱砂叶蝉的杀螨率达80%,化合物8f在50 mU g/m L时对棕榈蚜的杀灭活性达100%,化合物8R和8w在50 m g/m L浓度下对小菜蛾有100%的杀虫活性。此外,化合物8R(LC_(50)=19.61 mU/m L)和8W(LC_(50)=9.78 m u g/m L)对小菜蛾的杀虫活性与对照吡啶(LC_(50)=17.40 m g/m L)相当,甚至更好。(C)2016爱思唯尔有限公司。保留所有权利。
A new library of 1,3,4-thiadiazole-containing pyrazole oximes was designed and synthesized. Their acaricidal and insecticidal activities were evaluated. Bioassay results indicated that some target compounds exhibited good acaricidal and insecticidal properties. Especially, compound 8m had 80% acaricidal activity against Tetranychus cinnabarinus at the concentration of 50 mu g/mL, compound 8f displayed 100% insecticidal activities against Aphis craccivora at the concentration of 50 mu g/mL, compounds 8r and 8w showed 100% insecticidal activities against Plutella xylostella at the concentration of 50 mu g/mL. Furthermore, compounds 8r (LC50 = 19.61 mu g/mL) and 8w (LC50 = 9.78 mu g/mL) possessed comparable or even better insecticidal activities than the control Pyridalyl (LC50 = 17.40 mu g/mL) against P. xylostella. (C) 2016 Elsevier Ltd. All rights reserved.