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Discovery of N-Substituted Oseltamivir Derivatives as Potent and Selective Inhibitors of H5N1 Influenza Neuraminidase

文献类型： 外文期刊

作者： Xie, Yuanchao 1 ; Xu, Dongqing 1 ; Huang, Bing 2 ; Ma, Xiuli 2 ; Qi, Wenbao 3 ; Shi, Fangyuan 1 ; Liu, Xinyong 1 ; Zhang, 1 ;

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

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

3.South China Agr Univ, Coll Vet Med, Guangzhou 510642, Guangdong, Peoples R China

期刊名称：JOURNAL OF MEDICINAL CHEMISTRY （ 影响因子：7.446； 五年影响因子：7.319 ）

ISSN： 0022-2623

年卷期： 2014 年 57 卷 20 期

页码：

收录情况： SCI

摘要： To discover group-1-specific neuraminidase (NA) inhibitors that are especially involved in combating the H5N1 virus, two series of oseltamivir derivatives were designed and synthesized by targeting the 150-cavity. Among these, compound 20l was the most potent N1-selective inhibitor, with IC50 values of 0.0019, 0.0038, and 0.0067 mu M against NAs from three H5N1 viruses. These values are better than those of oseltamivir carboxylate. Compound 32 was another potent N1-selective inhibitor that exhibited a 12-fold increase in activity against the H274Y mutant relative to oseltamivir carboxylate. Molecular docking studies revealed that the 150-cavity was an auxiliary binding site that may contribute to the high selectivity of these compounds. The present work is a significant breakthrough in the discovery of potent group-1-specific neuraminidase inhibitors, which may be further investigated for the treatment of infection by the H5N1 virus.

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