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 anthra...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.展开更多
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)。
文摘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.
