Syntheses of triazole-modified zanamivir analogues via click chemistry and anti-AIV activities

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• 作者：Jian Li ; Mingyue Zheng ; Wei Tang ; Pei-Lan He ; Weiliang Zhu ; Tianxian Li ; Jian-Ping Zuo ; Hong Liu and Hualiang Jiang
• 关键词：Zanamivir analogues ; Avian influenza virus ; Click chemistry ; Molecular modeling
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：1 October 2006
• 年：2006
• 卷：16
• 期：19
• 页码：5009-5013
• 全文大小：265 K

文摘

Sixteen novel 4-triazole-modified zanamivir (1) analogues were synthesized using the click reactions, and their inhibitory activities against avian influenza virus (AIV, H5N1) were determined. Compound 3b exerts promising inhibitory activity with EC₅₀ of 6.4 μM, which is very close to that of zanamivir (EC₅₀ = 2.8 μM). Molecular modeling provided the information about the binding model between inhibitors and neuraminidase, which are in good agreement with inhibitory activities.