合成含卤吡唑苦参碱衍生物及其杀虫杀菌活性。
Synthesis of Halopyrazole Matrine Derivatives and Their Insecticidal and Fungicidal Activities.
机构信息
Institute of Natural Product Chemistry, College of Chemistry and Chemical Engineering/Key Laboratory of Green Prevention and Control on Fruits and Vegetables in South China, Ministry of Agriculture and Rural Affairs/Institute of Plant Health, Zhongkai University of Agriculture and Engineering, Guangzhou 510225, China.
Guangzhou Inspecting Testing and Certification Group Co., Ltd., Guangzhou 511447, China.
出版信息
Molecules. 2022 Aug 5;27(15):4974. doi: 10.3390/molecules27154974.
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 , and 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 , , and . 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.
苦参碱是一种传统的植物源农药，具有广谱的生物活性，在农业中得到了广泛的应用。成功地将卤代吡唑基团引入苦参碱的 C13 位，合成了 8 个新衍生物，产率为 78-87%。杀虫活性结果表明，引入卤代吡唑基团能显著提高苦参碱对 、 、 的杀虫活性，校正死亡率为 100%，比苦参碱高 25-65%。杀菌活性结果表明，衍生物对 、 、 有较高的抑制作用。其中，4-Cl-Pyr-Mat 效果最好，抑菌率比苦参碱高 23-33%。因此，引入卤代吡唑基团可以提高苦参碱的农业活性。
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