Isatin based Schiff bases as inhibitors of α-glucosidase: Synthesis, characterization, in vitro evaluation and molecular docking studies
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...
| Published in: | Bioorganic Chemistry |
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| Main Author: | |
| Format: | Article |
| Language: | English |
| Published: |
Academic Press Inc.
2015
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| Online Access: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-84928815461&doi=10.1016%2fj.bioorg.2015.03.005&partnerID=40&md5=113e06e633c17ccb7db89b098099d502 |
| Summary: | 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. © 2015 Elsevier Inc. All rights reserved. |
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| ISSN: | 452068 |
| DOI: | 10.1016/j.bioorg.2015.03.005 |