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通过点击化学合成三唑修饰的扎那米韦类似物及其抗禽流感病毒活性

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

作者信息

Li Jian, Zheng Mingyue, Tang Wei, He Pei-Lan, Zhu Weiliang, Li Tianxian, Zuo Jian-Ping, Liu Hong, Jiang Hualiang

机构信息

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.

出版信息

Bioorg Med Chem Lett. 2006 Oct 1;16(19):5009-13. doi: 10.1016/j.bmcl.2006.07.047. Epub 2006 Jul 28.

DOI:10.1016/j.bmcl.2006.07.047
PMID:16876409
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.

摘要

利用点击反应合成了16种新型4-三唑修饰的扎那米韦（1）类似物，并测定了它们对禽流感病毒（AIV，H5N1）的抑制活性。化合物3b表现出有前景的抑制活性，半数有效浓度（EC50）为6.4微摩尔，这与扎那米韦的EC50（2.8微摩尔）非常接近。分子模拟提供了抑制剂与神经氨酸酶之间结合模型的信息，这与抑制活性高度一致。

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