文献类型：期刊文献

中文题名：Synthesis of Triazole-Linked Amino Acid-Aryl C-Glycoside Hybrids via Click Chemistry as Novel PTPIB Inhibitors

英文题名：Synthesis of Triazole-Linked Amino Acid-Aryl C-Glycoside Hybrids via Click Chemistry as Novel PTPIB Inhibitors

作者：Wang, Jia[1];He, Xiaopeng[1];Gao, Lixin[2];Sheng, Li[2];Shi, Xiaoxin[1];Li, Jia[1];Chen, Guorong[1]

机构：[1]Key Laboratory for Advanced Materials and Institute of Fine Chemicals, and School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China;[2]National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes of Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China

年份：2011

卷号：29

期号：6

起止页码：1227

中文期刊名：Chinese Journal of Chemistry

外文期刊名：中国化学（英文版）

收录：CSTPCD;;Scopus;CSCD:【CSCD2011_2012】；

语种：英文

中文关键词：click chemistry;C-glycoside;triazolyl amino acid;PTP;inhibitors

外文关键词：click chemistry, C-glycoside, triazolyl amino acid, PTP, inhibitors

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 PTPlB inhibitors with low micromole-ranged inhibitory activity and at least several-fold selectivity over other homologous PTPs tested found crucial toward PTP1 B inhibition. In addition, the benzyl groups on glucosyl moiety were
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 PTPlB inhibitors with low micromole-ranged inhibitory activity and at least several-fold selectivity over other homologous PTPs tested found crucial toward PTP1 B inhibition. In addition, the benzyl groups on glucosyl moiety were