文献类型：期刊文献

中文题名：作为杀菌和杀虫先导的1,2,4-噁二嗪衍生物的设计与合成研究

英文题名：Design and Synthesis of 1,2,4-Oxadiazine Derivatives as Promising Fungicide and Insecticide Lead Compound

作者：章乐天[1];苏嘉媛[1];徐晓勇[1]

机构：[1]华东理工大学药学院上海市化学生物学(芳香杂环)重点实验室,上海200237

年份：2021

卷号：41

期号：9

起止页码：3539

中文期刊名：有机化学

外文期刊名：Chinese Journal of Organic Chemistry

收录：CSTPCD;;Scopus;WOS:【SCI-EXPANDED(收录号:WOS:000706836100015)】；北大核心:【北大核心2020】；CSCD:【CSCD2021_2022】；

基金：Project supported by the National Natural Science Foundation of China (No. 21672061), the National Key Research Program of China (No. 2017YFD0200505) and the Innovation Program of Shanghai Municipal Education Commission (No. 201701070002E00037).

语种：中文

中文关键词：噁二嗪;合成;生物电子等排;生物活性

外文关键词：oxadiazine;synthesis;bioisosterism;biological activities

摘要：噁二嗪片段常用于小分子的修饰和构象限制,同时噁二嗪也是一种理想的酰胺电子等排体.基于商品化琥珀酸脱氢酶抑制剂杀菌剂的结构框架,通过生物电子等排手段,以噁二嗪替换酰胺结构,设计并合成了24个1,2,4-噁二嗪类化合物.生物活性测试结果表明,在400 mg/L浓度下,大部分化合物对黄瓜霜霉病表现出较好的活性.此外,在600 mg/L的浓度下,这些化合物对粘虫的致死率达到100%,说明噁二嗪的结构值得作为先导继续研究,进而发现活性优异的新化合物.
Oxadiazine is an active fragment and usually is used for modification and conformation restriction of small molecules,meanwhile,it can be considered as an ideal and completely competent surrogate for the amide group.Based on the general framework of marketed succinate dehydrogenase inhibitors,twenty-four 1,2,4-oxadiazine compounds were designed and synthesized.The bioactivity test results showed that most of compounds exhibited good activities against Pseudoperonospora cubensis at 400 mg/L.In addition,the oxadiazine compounds have a 100%mortality against armyworms at 600 mg/L,which illustrates that oxadiazine structure is worth to be a lead compound and further modification to discover novel active with practical potentials.