抄録
A series of iso-allo-DNJ and L-isoDALDP derivatives were synthesized from dithioacetal 16 with sequential and highly diastereoselective Ho and Henry reactions, and aziridinium intermediate-mediated ring rearrangement as key steps. Glycosidase inhibition assay found four of them as selective α-glucosidase inhibitors, and the less substituted compound 30 showed more potent α-glucosidase inhibition (IC50 = 9.3 μM) than the others. Molecular docking study revealed different docking modes of the iso-allo-DNJ and L-isoDALDP derivatives from their parent compounds, and also the similarity of compound 30 to isofagomine.
本文言語 | 英語 |
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ページ(範囲) | 3453-3464 |
ページ数 | 12 |
ジャーナル | Organic and Biomolecular Chemistry |
巻 | 21 |
号 | 16 |
DOI | |
出版ステータス | 出版済み - 2023/04/26 |