Novel plant activators with thieno[2,3-d]-1,2,3-thiadiazole-6-carboxylate scaffold: Synthesis and bioactivity  

作　　者：Qing-Shan Du Yan-Xia Shi Peng-Fei Li Zhen-Jiang Zhao Wei-Ping Zhu Xu-Hong Qian Bao-Ju Li Yu-Fang Xu 

机构地区：[1]Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology [2]Institute of Vegetables and Flowers, Chinese Academy of Agricultural Sciences

出　　处：《Chinese Chemical Letters》2013年第11期967-969,共3页中国化学快报（英文版）

基　　金：financially supported by the National Basic Research Program of China (973 Program, No. 2010CB126100);the National High Technology Research and Development Program of China (863 Program, No. 2011AA10A207);the China 111 Project (No. B07023);the Fundamental Research Funds for the Central Universities.

摘　　要：The 1,2,3-thiadiazole-carboxylate moiety was reported to be an important pharmacophore of plant activators.In this study,a series of novel plant activators based on thieno[2,3-d]-1,2,3-thiadiazole-6-carboxylate were designed and synthesized and their biological activity as plant activators was studied.The structures of the novel compounds were identifed by1H NMR,19F NMR and HRMS.The in vivo bioassay showed that these novel compounds had good effcacy against seven plant diseases.Especially,compounds 1a and 1c were more potent than the commercialized plant activator BTH.Almost no fungicidal activity was observed for the active compounds in the in vitro assay,which matched the requirements as plant activators.The 1,2,3-thiadiazole-carboxylate moiety was reported to be an important pharmacophore of plant activators.In this study,a series of novel plant activators based on thieno[2,3-d]-1,2,3-thiadiazole-6-carboxylate were designed and synthesized and their biological activity as plant activators was studied.The structures of the novel compounds were identifed by1H NMR,19F NMR and HRMS.The in vivo bioassay showed that these novel compounds had good effcacy against seven plant diseases.Especially,compounds 1a and 1c were more potent than the commercialized plant activator BTH.Almost no fungicidal activity was observed for the active compounds in the in vitro assay,which matched the requirements as plant activators.

关 键 词：Thieno[2 3-d]-1 2 3-thiadiazole-6-carboxylate derivatives Plant activator Systemic acquired resistance 

分 类 号：TQ452[化学工程—农药化工]