含1,2,4-噁二唑噻唑类化合物的设计合成及生物活性  

Design,Synthesis and Biological Activity of 1,2,4-Oxadiazole Thiazole Compounds

作　　者：张如松 姜硕 朱宝玉 光明甲 王明慧[1] 许良忠[1] 孙鉴昕 Zhang Rusong;Jiang Shuo;Zhu Baoyu;Guang Mingjia;Wang Minghui;Xu Liangzhong;Sun Jianxin(College of Chemistry and Molecular Engineering of Qingdao University of Science and Technology,Qingdao 266042,China)

机构地区：[1]青岛科技大学化学与分子工程学院,山东青岛266042

出　　处：《山东化工》2023年第20期34-36,43,共4页Shandong Chemical Industry

摘　　要：为了解决目前的农药抗性问题,采用活性亚结构拼接法,以噁虫酮和噻虫嗪为先导化合物,设计合成了一系列含1,2,4-噁二唑噻唑类化合物,使用核磁共振波谱以及高分辨质谱确认了目标化合物的结构,并对目标化合物进行了杀二斑叶螨卵室内生物测试实验,结果表明,目标化合物对二斑叶螨卵的孵化均具有一定的抑制活性,其中目标化合物I4e在质量浓度为500 mg/L时,螨卵孵化抑制率为100%,在质量浓度为50 mg/L时,目标化合物I4a、I4b、I4e对二斑叶螨卵的孵化抑制率分别为64%,62%,77%。In order to solve the problem of pesticide resistance,a series of 1,2,4-oxadiazole thiazole compounds containing 1,2,4-oxadiazole were designed and synthesized by using oxazolone and thiamethoxam as lead compounds by active substructure splicing method.The structure of the target compounds was confirmed by nuclear magnetic resonance spectroscopy and high resolution mass spectrometry.The target compounds were tested in the laboratory biological test of Tetranychus urticae eggs.The results showed that the target compounds had certain inhibitory activity on the hatching of Tetranychus urticae eggs.The target compound I4e had a 100% inhibition rate on the hatching of Tetranychus urticae eggs at a mass concentration of 500 mg/L,and at a mass concentration of 50 mg/L.The hatching inhibition rates of target compounds I4a,I4b and I4e on T.urticae eggs were 64%,62% and 77%,respectively.

关 键 词：噁二唑 噻唑 合成 生物测试 

分 类 号：TQ453[化学工程—农药化工]