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Design, Synthesis, and Fungicidal Activities of Novel 5-Methyl-1H-1,2,3-trizole-4-carboxyl Amide Analogues.
Medicinal chemistry. Pub Date : 2015 Nov 12
Wang, Zhen-Jun, Yang, Hui-Hui, Tian, Lei, Zhao, Wei-Guang

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 N-benzyl-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 microg/mL) was lower than that of chlorothalonil (12.3 microg/mL).

中文翻译:

新型5-甲基-1H-1,2,3-三唑-4-羧基酰胺类似物的设计,合成和杀真菌活性。

琥珀酸脱氢酶抑制剂(SDHIs)是具有酰胺键的杀菌剂,广泛用于控制由植​​物病原性真菌引起的植物病害。由于新SDHI的广泛活动,它们引起了研究界的广泛关注。设计并合成了具有生物活性的1,2,3-三唑部分的一系列结构新颖的SDHI。生物活性筛选表明,某些设计的N-苯乙基-1,2,3-三唑-4-羧基酰胺类似物对菌核菌和灰葡萄孢表现出良好的杀真菌活性,而某些N-苄基1,2,3-三唑- 4-羧基酰胺类似物对辣椒疫霉和花生毛孢菌具有良好的杀真菌活性。化合物5d对花生空头孢菌的EC50值(6.6 microg / mL)低于百菌清(12.3 microg / mL)。
更新日期:2017-01-31
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