Syntheses of triazole-modified zanamivir analogues via click chemistry and anti-AIV activities |
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| Authors: | Li Jian Zheng Mingyue Tang Wei He Pei-Lan Zhu Weiliang Li Tianxian Zuo Jian-Ping Liu Hong Jiang Hualiang |
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| Institution: | Drug Discovery and Design Centre, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China. |
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| Abstract: | 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 EC(50) of 6.4 microM, which is very close to that of zanamivir (EC(50) = 2.8 microM). Molecular modeling provided the information about the binding model between inhibitors and neuraminidase, which are in good agreement with inhibitory activities. |
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