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Novel plant activators with thieno[2,3-d]-1,2,3-thiadiazole-6-carboxylate scaffold: Synthesis and bioactivity
Chinese Chemical Letters ( IF 9.4 ) Pub Date : 2013-11-01 , DOI: 10.1016/j.cclet.2013.07.003
Qing-Shan Du , Yan-Xia Shi , Peng-Fei Li , Zhen-Jiang Zhao , Wei-Ping Zhu , Xu-Hong Qian , Bao-Ju Li , Yu-Fang Xu

Abstract 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 identified by 1H NMR, 19F NMR and HRMS. The in vivo bioassay showed that these novel compounds had good efficacy 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.

中文翻译:

噻吩并[2,3-d] -1,2,3-噻二唑-6-羧酸盐骨架的新型植物活化剂:合成与生物活性

摘要据报道,1,2,3-噻二唑-羧酸酯部分是植物激活剂的重要药效团。在这项研究中,设计和合成了一系列基于噻吩并[2,3-d] -1,2,3-噻二唑-6-羧酸盐的新型植物活化剂,并研究了其作为植物活化剂的生物学活性。通过1 H NMR,19 F NMR和HRMS鉴定了新型化合物的结构。体内生物测定表明,这些新型化合物对七种植物病害均具有良好的功效。特别地,化合物1a和1c比商业化的植物活化剂BTH更有效。在体外测定中几乎没有观察到活性化合物的杀真菌活性,这符合作为植物活化剂的要求。
更新日期:2013-11-01
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