N-2 Alkylated analogues of aza-galactofagomine as potential inhibitors of β-glucosidase

Autor: Đurković Filip, Zlatović Mario, Sladić Dušan, Novaković Irena, Bihelović Filip, Ferjančić Zorana
Jazyk: angličtina
Rok vydání: 2024
Předmět:
Zdroj: Journal of the Serbian Chemical Society, Vol 89, Iss 10, Pp 1255-1267 (2024)
Druh dokumentu: article
ISSN: 0352-5139
1820-7421
DOI: 10.2298/JSC240315062D
Popis: The synthesis of four N-2-alkylated aza-galactofagomine (AGF) analogues was achieved by intermolecular reductive hydrazination or alkylation of suitably protected AGF. The synthesized compounds were evaluated as potential β-glucosidase inhibitors. The preliminary screening of inhibitor activity, conducted with sweet almond β-glucosidase immobilized in agar, as well as the standard inhibition assay with the same enzyme, showed the inhibitory potency of the synthesized analogues. In addition, these results are in a good agreement with the docking analysis of the human acid β-glucosidase, the enzyme implicated in Gaucher’s disease.
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