Chinese Journal of Organic Chemistry >
Design and Synthesis of 1,2,4-Oxadiazine Derivatives as Promising Fungicide and Insecticide Lead Compound
Received date: 2021-01-18
Revised date: 2021-03-26
Online published: 2021-06-07
Supported by
National Natural Science Foundation of China(21672061); National Key Research Program of China(2017YFD0200505); Innovation Program of Shanghai Municipal Education Commission(201701070002E00037)
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.
Key words： oxadiazine; synthesis; bioisosterism; biological activities
Letian Zhang , Jiayuan Su , Xiaoyong Xu . Design and Synthesis of 1,2,4-Oxadiazine Derivatives as Promising Fungicide and Insecticide Lead Compound[J]. Chinese Journal of Organic Chemistry, 2021 , 41(9) : 3539 -3549 . DOI: 10.6023/cjoc202101029
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