Design,synthesis and herbicidal activity study of aryl 2,6-disubstituted sulfonylureas as potent acetohydroxyacid synthase inhibitors |
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Authors: | Wei Wei Shaa Zhou Dandan Cheng Yuxin Li Jingbo Liu Yongtao Xie Yonghong Li Zhengming Li |
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Institution: | State Key Laboratory of Elemento-Organic Chemistry, Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Nankai University, No. 94, Weijin Road, Nankai District, Tianjin 300071, China |
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Abstract: | A series of sulfonylurea derivatives containing a 2,6-disubstituted aryl moiety were designed, synthesized and evaluated for their herbicidal activities. Most of these compounds showed excellent inhibitory rates against both monocotyledonous and dicotyledonous weeds, especially 10a, 10h and 10i. They exhibited equivalent or superior herbicidal efficiency than commercial chlorsulfuron at the dosage of 15 g/ha and the preliminary SAR was summarized. In order to illuminate the molecular mechanism of several potent compounds, their apparent inhibition constant (Kiapp) of Arabidopsis thaliana acetohydroxyacid synthase (AHAS) were determined and the results confirmed that these compounds were all potent AHAS inhibitors. 10i have a Kiapp of 11.5 nM, which is about 4 times as potent as chlorsulfuron (52.4 nM). |
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Keywords: | Sulfonylureas Acetohydroxyacid synthase (AHAS) Herbicidal activity Corresponding author at: Bo-Ling Building 518 Nankai University No 94 Weijin Road Tianjin 300071 China |
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