Synthesis and insecticidal evaluation of novel sulfide-containing amide derivatives as potential ryanodine receptor modulators  

作　　者：Yan Zhang Yuxin Li Huan Li Junfeng Shang Zhengming Li Baolei Wang 

机构地区：[1]State Key Laboratory of Elemento-Organic Chemistry,College of Chemistry,Nankai University,Tianjin 300071,China

出　　处：《Chinese Chemical Letters》2022年第1期501-507,共7页中国化学快报（英文版）

基　　金：Project supported by the National Key Research and Development Program of China(No.2017YFD0200505);the National Natural Science Foundation of China(Nos.21772103 and 31972287);Tianjin Natural Science Foundation(No.17JCYBJC19900)。

摘　　要：With the aim of discovering new bioactive pesticides for crop protection,a series of novel sulfidecontaining amide derivatives A were efficiently synthesized via a strategy of modifying the“amide”structure of anthranilic diamide insecticides.The single-crystal structures of A2-3 and A4-5 were firstly reported.The bioassay results showed that most of the synthesized compounds display moderate to high insecticidal activities.Particularly,some sulfone-containing compounds,e.g.,A2-3,A3-3 and A6-3,not only possessed favorable lethality rate(50%–100%)against P.xylostella at a concentration of 0.1 mg/L,but also held good activities towards a variety of agricultural pests such as M.separata,C.pipiens pallen,H.armigera and O.nubilalis;the larvicidal activities of A4-1 and A6-1 towards P.xylostella were close to that of chlorantraniliprole at 0.01 mg/L.The calcium imaging experiments revealed that the representative compounds A2-3 and A6-3 are potential ryanodine receptor(RyR)modulators.The structure–activity relationships were discussed in detail.These results provide useful information for further design and development of novel insecticides.

关 键 词：Sulfide-containing amide derivatives SULFOXIDE SULFONE Insecticidal activities Calcium channel 

分 类 号：TQ453[化学工程—农药化工]