Synthesis of multivalent difluorinated zanamivir analogs as potent antiviral inhibitors
文献类型：期刊论文
| 作者 | Yang, Zhao-Liang1; Zeng, Xiong-Fei1; Liu, Hai-Peng1; Yu, Qun1; Meng, Xin1; Yan, Zhong-Li2; Fan, Zhen-Chuan3,4; Xiao, Hai-Xia5; Iyer, Suri S.6; Yang, Yang1 |
| 刊名 | TETRAHEDRON LETTERS
 |
| 出版日期 | 2016-06-15 |
| 卷号 | 57期号:24页码:2579-2582 |
| 关键词 | Multivalent effect Difluorozanamivir Click chemistry Antiviral inhibitors |
| 英文摘要 | An efficient synthesis of mono-, di-, tetra-, and octa-valent difluorinated zanamivir analogs as potent inhibitors of influenza virus is reported. The mono difluorinated zanamivir with an azide linker attached at the C-7 position was synthesized in good yield from sialic acid using Selectfluor and (diethylaminosulfur trifluoride) DAST as the fluorination reagent. This key intermediate was attached on various alkynlated scaffolds via "Click Chemistry" to afford multivalent glycoclusters. A neuraminidase inhibition assay was used to evaluate the compounds for their inhibitory activity using H7N9 virus like particle. These multivalent sialosides show enhanced inhibition with IC50, values similar to 100-fold better than the monomer indicative of the strength of using a multivalent approach. (C) 2016 Elsevier Ltd. All rights reserved. |
| WOS标题词 | Science & Technology ; Physical Sciences |
| 类目[WOS] | Chemistry, Organic |
| 研究领域[WOS] | Chemistry |
| 关键词[WOS] | INFLUENZA-VIRUS NEURAMINIDASE ; DESIGN ; RESISTANCE ; INFECTION |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000377314700003 |
| 源URL | [http://124.16.173.210/handle/834782/2898]  |
| 专题 | 天津工业生物技术研究所_蛋白质工程与疫苗实验室 高福_期刊论文 |
| 作者单位 | 1.Tianjin Univ Sci & Technol, China Int Sci & Technol Cooperat Base Food Nut Sa, Sino French Joint Lab Food Nutr Safety & Med Chem, Key Lab Ind Fermentat Microbiol,Minist Educ,Coll, Tianjin 300457, Peoples R China 2.Tianjin Univ Sci & Technol, Res Ctr Modern Analyt Technol, Tianjin 300457, Peoples R China 3.Tianjin Univ Sci & Technol, Coll Food Engn & Biotechnol, Key Lab Food Nutr & Safety, Minist Educ, Tianjin 300457, Peoples R China 4.Obesita & Algaegen LLC, College Stn, TX 77845 USA 5.Chinese Acad Sci, Tianjin Inst Ind Biotechnol, Tianjin 300308, Peoples R China 6.Georgia State Univ, Ctr Diagnost & Therapeut, Dept Chem, Atlanta, GA 30302 USA |
| 推荐引用方式 GB/T 7714 | Yang, Zhao-Liang,Zeng, Xiong-Fei,Liu, Hai-Peng,et al. Synthesis of multivalent difluorinated zanamivir analogs as potent antiviral inhibitors[J]. TETRAHEDRON LETTERS,2016,57(24):2579-2582. |
| APA | Yang, Zhao-Liang.,Zeng, Xiong-Fei.,Liu, Hai-Peng.,Yu, Qun.,Meng, Xin.,...&Yu, Peng.(2016).Synthesis of multivalent difluorinated zanamivir analogs as potent antiviral inhibitors.TETRAHEDRON LETTERS,57(24),2579-2582. |
| MLA | Yang, Zhao-Liang,et al."Synthesis of multivalent difluorinated zanamivir analogs as potent antiviral inhibitors".TETRAHEDRON LETTERS 57.24(2016):2579-2582. |
入库方式： OAI收割
来源：天津工业生物技术研究所
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