N-2 Alkylated analogues of aza-galactofagomine as potential inhibitors of β-glucosidase
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, con...
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| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Serbian Chemical Society
2024-01-01
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| Series: | Journal of the Serbian Chemical Society |
| Subjects: | |
| Online Access: | https://doiserbia.nb.rs/img/doi/0352-5139/2024/0352-51392400062D.pdf |
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| Summary: | 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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| ISSN: | 0352-5139 1820-7421 |