| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1355097 | Bioorganic Chemistry | 2015 | 7 Pages |
•Synthesis of Isatin based Schiff bases.•In vitro α-glucosidase inhibitory activity.•Identification of a novel class of α-glucosidase inhibitors.•Structure–activity relationship established.•Molecular docking.
Isatin base Schiff bases (1–20) were synthesized, characterized by 1H NMR and EI/MS and evaluated for α-glucosidase inhibitory potential. Out of these twenty (20) compounds only six analogs showed potent α-glucosidase inhibitory potential with IC50 value ranging in between 2.2 ± 0.25 and 83.5 ± 1.0 μM when compared with the standard acarbose (IC50 = 840 ± 1.73 μM). Among the series compound 2 having IC50 value (18.3 ± 0.56 μM), 9 (83.5 ± 1.0 μM), 11 (3.3 ± 0.25 μM), 12 (2.2 ± 0.25 μM), 14 (11.8 ± 0.15 μM), and 20 (3.0 ± 0.15 μM) showed excellent inhibitory potential many fold better than the standard acarbose. The binding interactions of these active analogs were confirmed through molecular docking.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
