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

Authors :
Rahim, Fazal
Malik, Fazal
Ullah, Hayat
Wadood, Abdul
Khan, Fahad
Javid, Muhammad Tariq
Taha, Muhammad
Rehman, Wajid
Ur Rehman, Ashfaq
Khan, Khalid Mohammed
Source :
Bioorganic Chemistry. Jun2015, Vol. 60, p42-48. 7p.
Publication Year :
2015

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 IC 50 value ranging in between 2.2 ± 0.25 and 83.5 ± 1.0 μM when compared with the standard acarbose (IC 50 = 840 ± 1.73 μM). Among the series compound 2 having IC 50 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. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
00452068
Volume :
60
Database :
Academic Search Index
Journal :
Bioorganic Chemistry
Publication Type :
Academic Journal
Accession number :
102982946
Full Text :
https://doi.org/10.1016/j.bioorg.2015.03.005