| Study on the bioactivity changes of hydroxylated sulfonylureas derivatives: A possible metabolism |
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| 作者姓名： | Shu Rong Ban Cong Wei Niu Wen Bin Chen Zhi Hong Yu Si Wu Chen Wang Zhen Xi State-Key Laboratory of Elemento-Organic Chemistry |
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| 作者单位： | Shu Rong Ban，Cong Wei Niu，Wen Bin Chen，Zhi Hong Yu，Si Wu，Chen Wang，Zhen Xi State-Key Laboratory of Elemento-Organic Chemistry，Department of Chemical Biology，Nankai University，Tianjin 300071，China School of Pharmaceutical Science，Shanxi Medical University，Taiyuan 030001，China |
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| 基金项目： | 国家自然科学基金;国家重点基础研究发展计划(973计划) |
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| 摘 要： | Some new sulfonylureas and their hydroxylation products had been synthesized from 2-amino-4-methylpyrimidine. Their bioactivities against E. coli AHAS II in vitro were tested and the results indicated that the hydroxylation decreased the inhibition activities of sulfonylureas significantly. Subsequently herbicidal tests against stem-growth of barnyard grass and root-growth of rape confirmed the above conclusion. The preliminary molecular docking studies were also carried out to investigate the binding modes of non-hydroxylated and hydroxylated sulfonylureas with AHAS.
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| 关 键 词： | E. coli AHASⅡ |
Study on the bioactivity changes of hydroxylated sulfonylureas derivatives: A possible metabolism |
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| Shu Rong Ban,Cong Wei Niu,Wen Bin Chen,Zhi Hong Yu,Si Wu,Chen Wang,Zhen Xi State-Key Laboratory of Elemento-Organic Chemistry,.Study on the bioactivity changes of hydroxylated sulfonylureas derivatives: A possible metabolism[J].Chinese Chemical Letters,2007,18(2). |
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| Authors: | Shu Rong Ban Cong Wei Niu Wen Bin Chen Zhi Hong Yu Si Wu Chen Wang Zhen Xi |
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| Abstract: | Some new sulfonylureas and their hydroxylation products had been synthesized from 2-amino-4-methylpyrimidine. Their bioactivities against E. coli AHAS II in vitro were tested and the results indicated that the hydroxylation decreased the inhibition activities of sulfonylureas significantly. Subsequently herbicidal tests against stem-growth of barnyard grass and root-growth of rape confirmed the above conclusion. The preliminary molecular docking studies were also carried out to investigate the binding modes of non-hydroxylated and hydroxylated sulfonylureas with AHAS. |
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| Keywords: | Sulfonylureas Metabolism Hydroxylation Molecular docking |
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