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Preparation of triazole-linked glycosylated alpha-ketocarboxylic acid derivatives as new PTP1B inhibitors

文献类型：期刊论文

作者Song, Zhuo4; He, Xiao-Peng1,3; Li, Cui3; Gao, Li-Xin2; Wang, Zhao-Xia4; Tang, Yun3; Xie, Juan1; Li, Jia2; Chen, Guo-Rong4
刊名CARBOHYDRATE RESEARCH
出版日期2011-01-03
卷号346期号:1页码:140-145
关键词alpha-Ketocarboxylic acid Glycoconjugate Click reaction PTP1B inhibitor
ISSN号0008-6215
DOI10.1016/j.carres.2010.10.023
文献子类Article
英文摘要The synthesis of triazole-linked glycosyl acetophenone, benzoic acid, and alpha-ketocarboxylic acid derivatives was readily achieved via Cu(I)-catalyzed azide-alkyne cycloaddition ('click' reaction) in excellent yields of 93-97%. Among the synthesized glycoconjugates, the triazolyl alpha-ketocarboxylic acids were identified as the most potent protein tyrosine phosphatase 1B (FTP1B) inhibitors with micromole-ranged IC(50) values and moderate-to-good selectivity over a panel of homologous PTPs including TCPTP (4.6-fold), LAR (>30-fold), SHP-1 (>30-fold) and SHP-2 (>30-fold). Moreover, a docking simulation was conducted to propose a plausible binding mode of the glucosyl alpha-ketocarboxylic acid triazole with the enzymatic target. (C) 2010 Elsevier Ltd. All rights reserved.
WOS关键词TYROSINE-PHOSPHATASE 1B ; CLICK CHEMISTRY ; INSULIN SENSITIVITY ; GLYCOGEN-PHOSPHORYLASE ; COMPETITIVE INHIBITOR ; PROTEIN ; DISCOVERY ; POTENT ; MICE ; NUCLEOSIDE
资助项目National Natural Science Foundation of China[20876045] ; National Science & Technology Major Project of China 'Key New Drug Creation and Manufacturing Program[2009ZX09302-001] ; Shanghai Science and Technology Community[10410702700] ; Shanghai Science and Technology Community[08DZ2291300] ; Chinese Academy of Sciences[KSCX2-YW-R-168] ; French Embassy in Beijing, China[00000000]
WOS研究方向Biochemistry & Molecular Biology ; Chemistry
语种英语
WOS记录号WOS:000286715700018
出版者ELSEVIER SCI LTD
源URL[http://119.78.100.183/handle/2S10ELR8/278628]  
专题国家新药筛选中心
药物安全性评价中心
通讯作者Xie, Juan
作者单位1.CNRS, Inst Alembert, PPSM, ENS Cachan,UMR 8531, F-94235 Cachan, France;
2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China;
3.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China
4.E China Univ Sci & Technol, Key Lab Adv Mat & Fine Chem, Shanghai 200237, Peoples R China;
推荐引用方式
GB/T 7714		 Song, Zhuo,He, Xiao-Peng,Li, Cui,et al. Preparation of triazole-linked glycosylated alpha-ketocarboxylic acid derivatives as new PTP1B inhibitors[J]. CARBOHYDRATE RESEARCH,2011,346(1):140-145.
APA Song, Zhuo.,He, Xiao-Peng.,Li, Cui.,Gao, Li-Xin.,Wang, Zhao-Xia.,...&Chen, Guo-Rong.(2011).Preparation of triazole-linked glycosylated alpha-ketocarboxylic acid derivatives as new PTP1B inhibitors.CARBOHYDRATE RESEARCH,346(1),140-145.
MLA Song, Zhuo,et al."Preparation of triazole-linked glycosylated alpha-ketocarboxylic acid derivatives as new PTP1B inhibitors".CARBOHYDRATE RESEARCH 346.1(2011):140-145.

入库方式： OAI收割

来源：上海药物研究所

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