当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Click to a focused library of benzyl 6-triazolo(hydroxy)benzoic glucosides: novel construction of PTP1B inhibitors on a sugar scaffold.

Click to a focused library of benzyl 6-triazolo(hydroxy)benzoic glucosides: novel construction of PTP1B inhibitors on a sugar scaffold.

Abstract：

:With an aim of developing novel protein tyrosine phosphatase (PTP) 1B inhibitors based on sugar scaffolds, a focused library of benzyl 6-triazolo(hydroxy)benzoic glucosides was efficiently constructed via the modular and selective Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddtion (click chemistry). These glycoconjugates bearing alkyl chain length-varied bridges between the sugar and (hydroxy)-benzoic moieties were identified as new PTP1B inhibitors with selectivity over T-Cell PTP (TCPTP), SH2-Containing PTP-1 (SHP-1), SHP-2 and Leukocyte Antigen-Related Tyrosine Phosphatase (LAR). Molecular docking study sequentially elaborated the plausible binding modes of the structurally diverse sugar-based inhibitors with PTP1B.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Li C,He XP,Zhang YJ,Li Z,Gao LX,Shi XX,Xie J,Li J,Chen GR,Tang Y

doi

10.1016/j.ejmech.2011.06.025

subject

Has Abstract

pub_date

2011-09-01 00:00:00

pages

4212-8

issue

9

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(11)00501-0

journal_volume

46

pub_type

杂志文章

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