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Bioorg Chem. 2015 Jun;60:42-8. doi: 10.1016/j.bioorg.2015.03.005. Epub 2015 Apr 18.

Isatin based Schiff bases as inhibitors of α-glucosidase: Synthesis, characterization, in vitro evaluation and molecular docking studies.

Author information

1
Department of Chemistry, Hazara University, Mansehra 21120, Pakistan. Electronic address: fazalstar@gmail.com.
2
Department of Chemistry, Hazara University, Mansehra 21120, Pakistan.
3
Department of Biochemistry, Abdul Wali Khan University Mardan, Mardan 23200, Pakistan.
4
Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor, Malaysia; Faculty of Applied Science UiTM, 40450 Shah Alam, Selangor, Malaysia.
5
H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan.

Abstract

Isatin base Schiff bases (1-20) were synthesized, characterized by (1)H 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±1.0μM when compared with the standard acarbose (IC50=840±1.73μM). Among the series compound 2 having IC50 value (18.3±0.56μM), 9 (83.5±1.0μM), 11 (3.3±0.25μM), 12 (2.2±0.25μM), 14 (11.8±0.15μM), and 20 (3.0±0.15μM) showed excellent inhibitory potential many fold better than the standard acarbose. The binding interactions of these active analogs were confirmed through molecular docking.

KEYWORDS:

Isatin; Molecular docking; Schiff bases; Synthesis; α-Glucosidase inhibition

PMID:
25955493
DOI:
10.1016/j.bioorg.2015.03.005
[Indexed for MEDLINE]

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