Citation: 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. shu

Design, Synthesis and Biological Activity of Substituted-N-[4-(substituted-phenylsulfamoyl)phenyl]benzamide as Potential AHAS Inhibitors

State-Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071

Received Date: 1 September 2006

Fund Project: This project was supported by the National Basic Research Program of China (No. 2003CB114406), the Natural Science Foundation Program of China (No. 20602021) and the International Collaborative Key Program of Science and Technology Ministry of China (No. 2004DFA01500).

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.
- AHAS,
- molecular docking,
- organic synthesis,
- biological activity
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