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

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...

Full description

Bibliographic Details
Published in:Bioorganic Chemistry
Main Author: Rahim F.; Malik F.; Ullah H.; Wadood A.; Khan F.; Javid M.T.; Taha M.; Rehman W.; Ur Rehman A.; Khan K.M.
Format: Article
Language:English
Published: Academic Press Inc. 2015
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
id 2-s2.0-84928815461
spelling 2-s2.0-84928815461
Rahim F.; Malik F.; Ullah H.; Wadood A.; Khan F.; Javid M.T.; Taha M.; Rehman W.; Ur Rehman A.; Khan K.M.
Isatin based Schiff bases as inhibitors of α-glucosidase: Synthesis, characterization, in vitro evaluation and molecular docking studies
2015
Bioorganic Chemistry
60

10.1016/j.bioorg.2015.03.005
https://www.scopus.com/inward/record.uri?eid=2-s2.0-84928815461&doi=10.1016%2fj.bioorg.2015.03.005&partnerID=40&md5=113e06e633c17ccb7db89b098099d502
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.
Academic Press Inc.
452068
English
Article
author Rahim F.; Malik F.; Ullah H.; Wadood A.; Khan F.; Javid M.T.; Taha M.; Rehman W.; Ur Rehman A.; Khan K.M.
spellingShingle Rahim F.; Malik F.; Ullah H.; Wadood A.; Khan F.; Javid M.T.; Taha M.; Rehman W.; Ur Rehman A.; Khan K.M.
Isatin based Schiff bases as inhibitors of α-glucosidase: Synthesis, characterization, in vitro evaluation and molecular docking studies
author_facet Rahim F.; Malik F.; Ullah H.; Wadood A.; Khan F.; Javid M.T.; Taha M.; Rehman W.; Ur Rehman A.; Khan K.M.
author_sort Rahim F.; Malik F.; Ullah H.; Wadood A.; Khan F.; Javid M.T.; Taha M.; Rehman W.; Ur Rehman A.; Khan K.M.
title Isatin based Schiff bases as inhibitors of α-glucosidase: Synthesis, characterization, in vitro evaluation and molecular docking studies
title_short Isatin based Schiff bases as inhibitors of α-glucosidase: Synthesis, characterization, in vitro evaluation and molecular docking studies
title_full Isatin based Schiff bases as inhibitors of α-glucosidase: Synthesis, characterization, in vitro evaluation and molecular docking studies
title_fullStr Isatin based Schiff bases as inhibitors of α-glucosidase: Synthesis, characterization, in vitro evaluation and molecular docking studies
title_full_unstemmed Isatin based Schiff bases as inhibitors of α-glucosidase: Synthesis, characterization, in vitro evaluation and molecular docking studies
title_sort Isatin based Schiff bases as inhibitors of α-glucosidase: Synthesis, characterization, in vitro evaluation and molecular docking studies
publishDate 2015
container_title Bioorganic Chemistry
container_volume 60
container_issue
doi_str_mv 10.1016/j.bioorg.2015.03.005
url https://www.scopus.com/inward/record.uri?eid=2-s2.0-84928815461&doi=10.1016%2fj.bioorg.2015.03.005&partnerID=40&md5=113e06e633c17ccb7db89b098099d502
description 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.
publisher Academic Press Inc.
issn 452068
language English
format Article
accesstype
record_format scopus
collection Scopus
_version_ 1809678486747480064

Similar Items