Synthesis of Triazole-Linked Amino Acid-Aryl C-Glycoside Hybrids via Click Chemistry as Novel PTP1B Inhibitors
文献类型：期刊论文
| 作者 | Wang Jia2,3,4 ; He Xiaopeng2,3,4; Gao Lixin1; Sheng Li1; Shi Xiaoxin2,3,4; Li Jia1; Chen Guorong2,3,4
|
| 刊名 | CHINESE JOURNAL OF CHEMISTRY
 |
| 出版日期 | 2011-06 |
| 卷号 | 29期号:6页码:1227-1232 |
| 关键词 | click chemistry C-glycoside triazolyl amino acid PTP inhibitors |
| ISSN号 | 1001-604X |
| DOI | 10.1002/cjoc.201190228 |
| 文献子类 | Article |
| 英文摘要 | Triazolyl phenylalanine and tyrosine-aryl C-glycoside hybrids were readily synthesized via microwave-assisted Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition in high yields. Successive enzymatic assay identified the synthesized glycoconjugates as novel PTP1B inhibitors with low micromole-ranged inhibitory activity and at least several-fold selectivity over other homologous PTPs tested. In addition, the benzyl groups on glucosyl moiety were found crucial toward PTP1B inhibition. |
| WOS关键词 | TYROSINE-PHOSPHATASE 1B ; INSULIN SENSITIVITY ; CYCLOADDITION ; DISCOVERY ; MICE ; BINDING ; OBESITY ; DESIGN ; PROBES ; DRUG |
| 资助项目 | National Natural Science Foundation of China[20876045] ; National Natural Science Foundation of China[30801405] ; National Basic Research Program of China[2007CB914201] ; National Science & Technology Major Project of China[2009ZX09302-001] ; Shanghai Science and Technology Community[10410702700] ; Shanghai Science and Technology Community[09DZ2291200] ; Chinese Academy of Sciences[KSCX2-YW-R-168] ; Fundamental Research Funds for the Central Universities[WK1013002] ; French Embassy in Beijing, P. R. China[00000000] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| CSCD记录号 | CSCD:4248096 |
| WOS记录号 | WOS:000292215300025 |
| 出版者 | WILEY-V C H VERLAG GMBH |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278518]  |
| 专题 | 国家新药筛选中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物安全性评价中心 |
| 通讯作者 | Li Jia |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening,State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.E China Univ Sci & Technol, Key Lab Adv Mat, Shanghai 200237, Peoples R China; 3.E China Univ Sci & Technol, Inst Fine Chem, Shanghai 200237, Peoples R China; 4.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang Jia,He Xiaopeng,Gao Lixin,et al. Synthesis of Triazole-Linked Amino Acid-Aryl C-Glycoside Hybrids via Click Chemistry as Novel PTP1B Inhibitors[J]. CHINESE JOURNAL OF CHEMISTRY,2011,29(6):1227-1232. |
| APA | Wang Jia.,He Xiaopeng.,Gao Lixin.,Sheng Li.,Shi Xiaoxin.,...&Chen Guorong.(2011).Synthesis of Triazole-Linked Amino Acid-Aryl C-Glycoside Hybrids via Click Chemistry as Novel PTP1B Inhibitors.CHINESE JOURNAL OF CHEMISTRY,29(6),1227-1232. |
| MLA | Wang Jia,et al."Synthesis of Triazole-Linked Amino Acid-Aryl C-Glycoside Hybrids via Click Chemistry as Novel PTP1B Inhibitors".CHINESE JOURNAL OF CHEMISTRY 29.6(2011):1227-1232. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。