新型含吡唑环结构的吡唑肟酯类化合物的合成与生物活性研究  

Synthesis and Biological Activities of Novel Pyrazole Oxime Esters Containing Substituted Pyrazolyl Group

作　　者：戴红[1,2] 黄美岭 葛书山 孙思宇 沈爱宝 成晓燕[1] 李春建[3] 石健[3] 

机构地区：[1]南通大学化学化工学院,南通226019 [2]南通大学药学院,南通226001 [3]南通大学分析测试中心,南通226019

出　　处：《有机化学》2017年第12期3289-3295,共7页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.21372135);江苏省"六大人才高峰"(No.2013-SWYY-013);南通市科技计划(No.MS22015020)资助项目~~

摘　　要：为了寻找与发现具有优良生物活性的吡唑肟类衍生物,采用活性亚结构拼接方法,设计并合成了一系列未见文献报道的新型含取代吡唑环结构的吡唑肟酯类化合物.通过~1H NMR,^(13)C NMR和元素分析等方法确证了目标化合物的结构.初步的生物活性测试结果表明,在测试浓度为500μg/m L时,部分化合物对蚜虫表现出较好的杀灭活性,部分化合物对褐飞虱显示出较好的杀灭作用.另外,部分化合物还对HepG2细胞呈现出一定的抗肿瘤活性.In order to explore novel pyrazole derivatives with good biological activities, a series of pyrazole-containing pyrazole oxime esters were designed and synthesized according to the method of active substructure combination. Their structures were determined by ~1H NMR, ^（13）C NMR spectra and elemental analysis. The preliminary bioactivity test showed that some of the target compounds had good insecticidal activity against Aphis medicaginis at a concentration of 500 μg/m L, some title compounds displayed good insecticidal activity against Nilaparvata lugens at 500 μg/m L. In addition, some of the designed compounds exhibited certain anti-tumor activity against Hep G2 cells.

关 键 词：吡唑 吡唑肟 合成 生物活性 

分 类 号：O626.21[理学—有机化学]