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新型5-甲基-1H-1,2,3-三唑-4-甲酰胺类似物的设计、合成及杀菌活性

Design, Synthesis, and Fungicidal Activities of Novel 5-Methyl-1H-1,2,3- trizole-4-carboxyl Amide Analogues.

作者信息

Wang Zhen-Jun, Yang Hui-Hui, Tian Lei, Zhao Wei-Guang

机构信息

Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin, 300071, China.

出版信息

Med Chem. 2016;12(3):290-5. doi: 10.2174/1573406412666151112125006.

Abstract

Succinate dehydrogenase inhibitors (SDHIs) are fungicides with an amide bond widely used to control plant diseases caused by phytopathogenic fungi. Because of broad spectrum activity of new SDHIs, they have attracted wide attention from the research community. A series of structurally novel SDHIs with a bioactive 1,2,3-triazole moiety were designed and synthesized. Bioactivity screening showed that some of designed N-phenethyl-1,2,3-trizole-4-carboxyl amide analogues exhibited good fungicidal activities toward Sclerotinia sclerotiorum and Botrytis cinerea, while some of Nbenzyl- 1,2,3-trizole-4-carboxyl amide analogues exhibited good fungicidal activities toward Phytophthora capsici and Cercospora arachidicola. EC50 value of compound 5d against Cercospora arachidicola (6.6 µg/mL) was lower than that of chlorothalonil (12.3 µg/mL).

摘要

琥珀酸脱氢酶抑制剂(SDHIs)是一类带有酰胺键的杀菌剂,广泛用于防治由植物病原真菌引起的植物病害。由于新型SDHIs具有广谱活性,它们已引起了研究界的广泛关注。设计并合成了一系列具有生物活性的1,2,3-三唑部分的结构新颖的SDHIs。生物活性筛选表明,一些设计的N-苯乙基-1,2,3-三唑-4-羧酰胺类似物对核盘菌和灰葡萄孢表现出良好的杀菌活性,而一些N-苄基-1,2,3-三唑-4-羧酰胺类似物对辣椒疫霉和花生尾孢表现出良好的杀菌活性。化合物5d对花生尾孢的EC50值(6.6 µg/mL)低于百菌清(12.3 µg/mL)。

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