Citation: Shu Rong Ban, Cong Wei Niu, Wen Bin Chen, Zhi Hong Yu, Si Wu, Chen Wang, Zhen Xi. Study on the bioactivity changes of hydroxylated sulfonylureas derivatives:A possible metabolism[J]. Chinese Chemical Letters, ;2007, 18(2): 205-208. doi: 10.1016/j.cclet.2006.12.012 shu

Study on the bioactivity changes of hydroxylated sulfonylureas derivatives:A possible metabolism

Shu Rong Ban ^a,b, ,
Cong Wei Niu ^a ,
Wen Bin Chen ^a ,
Zhi Hong Yu ^a ,
Si Wu ^a ,
Chen Wang ^a ,
Zhen Xi ^a

a State-Key Laboratory of Elemento-Organic Chemistry, Department of Chemical Biology, Nankai University, Tianjin 300071, China;
b School of Pharmaceutical Science, Shanxi Medical University, Taiyuan 030001, China

Received Date: 14 September 2006

Fund Project: We are grateful to the National Natural Science Foundation of China (No. 20432010) and National Basic Research Program of China (973) (No. 2003CB114400) for the financial support.

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.
- Sulfonylureas,
- Metabolism,
- Hydroxylation,
- E.coli AHASⅡ,
- Molecular docking
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