Application of click chemistry towards an efficient synthesis of 1,2,3-1H-triazolyl glycohybrids as enzyme inhibitors

被引:62
作者
Anand, Namarata [1 ]
Jaiswal, Natasha [2 ]
Pandey, Sarvesh Kumar [1 ]
Srivastava, A. K. [2 ]
Tripathi, Rama P. [1 ]
机构
[1] Cent Drug Res Inst CSIR, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
[2] Cent Drug Res Inst CSIR, Div Biochem, Lucknow 226001, Uttar Pradesh, India
关键词
Click chemistry; CuAAC; Glycosyl triazoles; alpha-Glucosidase; Glucose-6-phosphatase; Glycogen phosphorylase; ESCHERICHIA-COLI; BIOLOGICAL EVALUATION; MAMMALIAN GALECTINS; TRIAZOLES; ADHESION; BINDING; AZIDE; 1,2,3-TRIAZOLES; DERIVATIVES; ALKYNES;
D O I
10.1016/j.carres.2010.10.017
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
An efficient synthesis of novel 1,2,3-1H-triazolyl glycohybrids with two or more than two sugar units or a chromenone moiety via copper-catalysed azide-alkyne cycloaddition (CuAAC), a 1,3-dipolar cycloaddition of glycosyl azides to 2,3-unsaturated alkynyl glycosides or propargyloxy coumarins is described. The synthesised glycohybrids were screened for their a-glucosidase, glycogen phosphorylase and glucose-6-phosphatase inhibitory activities. A few of the glycohybrids showed promising inhibitory activities against these enzymes. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码:16 / 25
页数:10
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