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

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

引用本文: 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
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

  • 基金项目:

    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.

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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  • 收稿日期:  2006-09-14
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