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Further discovery of caffeic acid derivatives as novel influenza neuraminidase inhibitors

文献类型： 外文期刊

作者： Xie, Yuanchao 1 ; Huang, Bing 2 ; Yu, Kexiang 2 ; Xu, Wenfang 1 ;

作者机构： 1.Shandong Univ, Dept Med Chem, Sch Pharmaceut Sci, Jinan 250012, Shandong, Peoples R China

2.Shandong Acad Agr Sci, Inst Poultry Sci, Jinan 250023, Shandong, Peoples R China

关键词： Caffeic acid;Influenza;Inhibitor;Neuraminidase

期刊名称：BIOORGANIC & MEDICINAL CHEMISTRY （ 影响因子：3.641； 五年影响因子：3.319 ）

ISSN：

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收录情况： SCI

摘要： Eight series of compounds, each series containing two to five compounds were prepared by structural modifications of a lead, which was previously discovered as a mild influenza neuraminidase (NA) inhibitor. On the basis of the biological result, a detailed structure-activity relationship (SAR) was derived and discussed. Several caffeic acid derivatives that acted as non-competitive inhibitors were close or superior to the lead and also presented good antiviral activities in cells. Besides, it was interesting to find that modifications of the lead with different strategies could result in selective inhibition against N1 or N2. The preliminary docking analysis indicated that the 150-cavity of the enzymes played an important role in the selective inhibition.

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