869957-40-4Relevant academic research and scientific papers
1H-1,2,3-Triazol-1-yl thiodigalactoside derivatives as high affinity galectin-3 inhibitors
Salameh, Bader A.,Cumpstey, Ian,Sundin, Anders,Leffler, Hakon,Nilsson, Ulf J.
experimental part, p. 5367 - 5378 (2010/09/05)
Galactose C3-triazole derivatives were synthesized by Cu(I)-catalyzed cycloaddition between acetylenes and galactose C3-azido derivatives. Evaluation against galectin-3, 7, 8N (N-terminal) and 9N (N-terminal) revealed 1,4-disubstituted triazoles to be high-affinity inhibitors of galectin-3 with selectivity over galectin-7, 8N, and 9N. Conformational analysis of 1,4-di- and 1,4,5-tri-substituted galactose C3-triazoles suggested that a triazole C5-substituent interfered sterically with the galectin proteins, which explained their poor affinities compared to the corresponding 1,4-disubstituted triazoles. Introduction of two 1,4-disubstituted triazole moieties onto thiodigalactoside resulted in affinities down to 29 nM for galectin-3.
NOVEL 3-TRIAZOLYL-GALACTOSIDE INHIBITORS OF GALECTINS
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Page/Page column 20-21; 26-27; 29, (2008/06/13)
The present invention relates to novel 3-triazolyl-galactosides, the use of said triazolyl-galactosides as medicament as well as for the manufacture of a medicament for treatment of disorders relating to the binding of galactin to receptors in a mammal. S
