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Synthesis and Evaluation of Novel N-(4'-Arylpyrimidin-2'-yl) Sulfonylurea Derivatives as Potential Antifungal Agents

Synthesis and Evaluation of Novel N-(4'-Arylpyrimidin-2'-yl) Sulfonylurea Derivatives as Potential Antifungal Agents
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摘要 Sulfonylureas(SUs) are potent and selective inhibitors of acetohydroxyacid synthase and has been used as herbicides. Some SUs also displayed other biological activities. In order to discuss the antifungal activity of SUs, a series of novel SUs containing aryl-substituted pyrimidine moieties was designed and synthesized. The preliminary bioassay showed that the title compounds exhibited moderate to favorable fungicidal activities in vivo. Especially, compound 9b exhibited more efficacy than the controls against five fungi at 25 mg/L. These promising results indicate that an aryl group on pyrimidine ring is favorable for antifungal activity and SUs are potential inhibitors for some phytopathogenic fungi. Sulfonylureas(SUs) are potent and selective inhibitors of acetohydroxyacid synthase and has been used as herbicides. Some SUs also displayed other biological activities. In order to discuss the antifungal activity of SUs, a series of novel SUs containing aryl-substituted pyrimidine moieties was designed and synthesized. The preliminary bioassay showed that the title compounds exhibited moderate to favorable fungicidal activities in vivo. Especially, compound 9b exhibited more efficacy than the controls against five fungi at 25 mg/L. These promising results indicate that an aryl group on pyrimidine ring is favorable for antifungal activity and SUs are potential inhibitors for some phytopathogenic fungi.
出处 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2015年第2期218-223,共6页 高等学校化学研究(英文版)
基金 Supported by the National Natural Science Foundation of China(No.21272129) and the National Key Technologies R&D Program of China(No.2011BAE06B05).
关键词 Acetohydroxyacid synthase SULFONYLUREA Fungicidal activity Substituted pyrimidine Acetohydroxyacid synthase Sulfonylurea Fungicidal activity Substituted pyrimidine
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