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

doi:10.1007/s40242-015-4362-5

Chemical Research in Chinese Universities ›› 2015, Vol. 31 ›› Issue (2): 218-223.doi: 10.1007/s40242-015-4362-5

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

CHEN Wei^1,2, LI Yuxin^1,2, SHI Yanxia³, WEI Wei^1,2, CHEN Youwei^1,2, LI Yonghong¹, LIU Jingbo^1,2, LI Baoju³, LI Zhengming^1,2

1. State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, P. R. China;
2. Collaborative Innovation Center of Chemical Science and Engineering(Tianjin), Nankai University, Tianjin 300071, P. R. China;
3. Institute of Vegetables and Flowers, Chinese Academy of Agricultural Sciences, Beijing 100081, P. R. China

Received:2014-09-28 Revised:2015-01-22 Online:2015-04-01 Published:2015-01-26
Contact: LI Baoju, LI Zhengming E-mail:nkzml@vip.163.com;libj@mail.coas.net.cn
Supported by:
Supported by the National Natural Science Foundation of China(No.21272129) and the National Key Technologies R&D Program of China(No.2011BAE06B05).

Abstract

Abstract:

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.

Key words: Acetohydroxyacid synthase, Sulfonylurea, Fungicidal activity, Substituted pyrimidine

CHEN Wei, LI Yuxin, SHI Yanxia, WEI Wei, CHEN Youwei, LI Yonghong, LIU Jingbo, LI Baoju, LI Zhengming. Synthesis and Evaluation of Novel N-(4'-Arylpyrimidin-2'-yl) Sulfonylurea Derivatives as Potential Antifungal Agents[J]. Chemical Research in Chinese Universities, 2015, 31(2): 218-223.

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

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