Syntheses of triazole-modified zanamivir analogues via click chemistry and anti-AIV activities
Syntheses of triazole-modified zanamivir analogues via click chemistry and anti-AIV activities
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DOI：
10.1016/j.bmcl.2006.07.047
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发表时间：
2006-10-01
影响因子：
2.7
通讯作者：
Jiang, Hualiang
中科院分区：
文献类型：
--
作者：
Li, Jian;Zheng, Mingyue;Jiang, Hualiang
通过点击反应合成了16个4-三氮唑修饰的扎那米韦(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具有良好的抑制活性，其EC50为6.4mU M，与扎那米韦相近(EC50=2.8mU M)。分子模拟提供了抑制剂与神经氨酸酶结合模式的信息，与抑制活性吻合较好。(C)2006爱思唯尔有限公司。保留所有权利。
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 mu M, which is very close to that of zanamivir (EC50 = 2.8 mu M). Molecular modeling provided the information about the binding model between inhibitors and neuraminidase, which are in good agreement with inhibitory activities. (c) 2006 Elsevier Ltd. All rights reserved.