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首页> 外文期刊>Bioorganic and medicinal chemistry >Binding of triazole-linked galactosyl arylsulfonamides to galectin-3 affects Trypanosoma cruzi cell invasion
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Binding of triazole-linked galactosyl arylsulfonamides to galectin-3 affects Trypanosoma cruzi cell invasion

机译：Binding of triazole-linked galactosyl arylsulfonamides to galectin-3 affects Trypanosoma cruzi cell invasion

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Graphical abstract Display Omitted Abstract The synthesis of the O-3 triazole-linked galactosyl arylsulfonamides 1 – 7 as potential inhibitors of Trypanosoma cruzi cell invasion is described. These target compounds were synthesized by Cu(I)-catalysed azide-alkyne cycloaddition reaction (‘click chemistry’) between different azide arylsulfonamides and the alkyne-based sugar 3-O-propynyl-βGalOMe. Inhibition assays of T. cruzi cell invasion with compounds 1 – 7 showed reduced values of infection index (～20) for compounds 3 and 5 , bearing the corresponding 5-methylisoxazole and 2,4-dimethoxypyrimidine groups, which also presented higher binding affinities to galectin-3 (EC 50 17–18?μM) in Corning Epic label-free assays. In agreement with experimental results, the assessment of the theoretical binding of compounds 1 – 7 to galectin-3 by MM/PBSA method displayed higher affinities for compounds 3 (?9.7?kcal/mol) and 5 (?11.1?kcal/mol). Overall, these achievements highlight compounds 3 and 5 as potential T. cruzi cell invasion blockers by means of a galectin-3 binding-related mechanism, revealing galectin-3 as an important host target for design of novel anti-trypanosomal agents.

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