Microwave-Accelerated Click Chemistry: Expeditious Synthesis of Novel Triazole-linked Salicylic beta-D-O-Glycosides with PTP1B Inhibitory Activity | |
Yang, Jin-Wei1,5; Li, Cui2; He, Xiao-Peng2,3; Zhao, Hong1,5; Gao, Li-Xin4; Zhang, Wei4; Shi, Xiao-Xin2; Tang, Yun2; Li, Jia4; Chen, Guo-Rong1,5 | |
刊名 | BULLETIN OF THE KOREAN CHEMICAL SOCIETY |
2010-11-20 | |
卷号 | 31期号:11页码:3359-3365 |
关键词 | Click chemistry Microwave irradiation Carbohydrate-based drug discovery PTP1B inhibitor Docking simulation |
ISSN号 | 0253-2964 |
DOI | 10.5012/bkcs.2010.31.11.3359 |
文献子类 | Article |
英文摘要 | The incorporation of microwave irradiation with the prevalent "click chemistry" is currently of considerable synthetic interest We describe here the introduction of such laboratorial shortcut into carbohydrate-based drug discovery, resulting in the rapid formation of a series of triazole-linked salicylic beta-D-O-glycosides with biological activities All "clicked" products were achieved in excellent yields (approximate to 90%) within only a quarter In addition, based on the structural characteristics of the afforded glycomimetics, their inhibitory activities were evaluated toward protein tyrosine phosphatases 1B (PTP1B) and a panel of homologous protein tyrosine phosphatases (PTPs) Docking simulation A as also conducted to plausibly propose binding modes of this glycosyl salicylate series with the enzymatic target |
资助项目 | National Natural Science Foundation of China[20876045] ; National Science & Technology Major Project of China[2009 ZX09302-001] ; Shanghai Science and Technology Community[10410702700] ; Shanghai Science and Technology Community[08DZ2291300] ; Chinese Academy of Sciences[KSCX2-YW-R-168] ; French Embassy in China[00000000] |
WOS关键词 | TYROSINE-PHOSPHATASE 1B ; MEDICAL APPLICATIONS ; ACID ; DISCOVERY ; SCAFFOLDS ; DRUGS |
WOS研究方向 | Chemistry |
语种 | 英语 |
出版者 | KOREAN CHEMICAL SOC |
WOS记录号 | WOS:000284794100055 |
内容类型 | 期刊论文 |
源URL | [http://119.78.100.183/handle/2S10ELR8/278716] |
专题 | 国家新药筛选中心 药物安全性评价中心 |
通讯作者 | Li, Jia |
作者单位 | 1.E China Univ Sci & Technol, Key Lab Adv Mat, Shanghai 200237, Peoples R China; 2.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China; 3.CNRS, ENS Cachan, PPSM, F-94230 Cachan, France 4.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; 5.E China Univ Sci & Technol, Inst Fine Chem, Shanghai 200237, Peoples R China; |
推荐引用方式 GB/T 7714 | Yang, Jin-Wei,Li, Cui,He, Xiao-Peng,et al. Microwave-Accelerated Click Chemistry: Expeditious Synthesis of Novel Triazole-linked Salicylic beta-D-O-Glycosides with PTP1B Inhibitory Activity[J]. BULLETIN OF THE KOREAN CHEMICAL SOCIETY,2010,31(11):3359-3365. |
APA | Yang, Jin-Wei.,Li, Cui.,He, Xiao-Peng.,Zhao, Hong.,Gao, Li-Xin.,...&Chen, Guo-Rong.(2010).Microwave-Accelerated Click Chemistry: Expeditious Synthesis of Novel Triazole-linked Salicylic beta-D-O-Glycosides with PTP1B Inhibitory Activity.BULLETIN OF THE KOREAN CHEMICAL SOCIETY,31(11),3359-3365. |
MLA | Yang, Jin-Wei,et al."Microwave-Accelerated Click Chemistry: Expeditious Synthesis of Novel Triazole-linked Salicylic beta-D-O-Glycosides with PTP1B Inhibitory Activity".BULLETIN OF THE KOREAN CHEMICAL SOCIETY 31.11(2010):3359-3365. |
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