| Design, Synthesis and Biological Activity of Substituted-N-[4-（substituted-phenylsulfamoyl）phenyl]benzamide as Potential AHAS Inhibitors |
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| 引用本文： | Jian Guo WANC Yong Jun XIAO Yong Hong LI Xing Hai LIU Zheng Ming LI. Design, Synthesis and Biological Activity of Substituted-N-[4-（substituted-phenylsulfamoyl）phenyl]benzamide as Potential AHAS Inhibitors[J]. 中国化学快报, 2006, 17(12): 1555-1558 |
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| 作者姓名： | Jian Guo WANC Yong Jun XIAO Yong Hong LI Xing Hai LIU Zheng Ming LI |
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| 作者单位： | Jian Guo WANG，Yong Jun XIAO，Yong Hong LI，Xing Hai LIU，Zheng Ming LI? State-Key Laboratory of Elemento-Organic Chemistry，Nankai University，Tianjin 300071 |
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| 基金项目： | 国家重点基础研究发展计划(973计划);国家自然科学基金 |
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| 摘 要： | Acetohydroxyacid synthase (AHAS) is an ideal target for the design of environmental benign herbicides, because it catalyzes the first step in the biosynthesis of branched chain amino acids, which does not exist in mammal bodies1-4. Typical AHAS inhibitors…
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| 关 键 词： | 乙酰羟酸合成酶抑制剂 AHAS 分子对接 有机合成 生物学活性 除草剂 |
| 收稿时间： | 2006-09-01 |
Design, Synthesis and Biological Activity of Substituted-N-[4- (substituted-phenylsulfamoyl)phenyl]benzamide as Potential AHAS Inhibitors |
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| Jian Guo WANG,Yong Jun XIAO,Yong Hong LI,Xing Hai LIU,Zheng Ming LI. Design, Synthesis and Biological Activity of Substituted-N-[4- (substituted-phenylsulfamoyl)phenyl]benzamide as Potential AHAS Inhibitors[J]. Chinese Chemical Letters, 2006, 17(12): 1555-1558 |
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| Authors: | Jian Guo WANG Yong Jun XIAO Yong Hong LI Xing Hai LIU Zheng Ming LI |
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| Abstract: | Based on the crystal structure of AHAS/sulfonylurea complex, we obtained 296 compounds with low binding energy towards AHAS via virtual screening. One series of them have been synthesized. Preliminary bioassay indicated that some compounds displayed good herbicidal activity on rape and barnygrass and inhibited AHAS to some extent. This study indicated the rationality of our molecular design based on the crystal structure of target enzyme. |
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| Keywords: | AHAS molecular docking organic synthesis biological activity. |
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