Synthesis, in vitro evaluation and molecular docking studies of thiazole derivatives as new inhibitors of α-glucosidase

Synthesis, in vitro evaluation and molecular docking studies of thiazole derivatives as new inhibitors of α-glucosidase

A series of thiazole derivatives 1-21 were prepared, characterized by EI-MS and 1H NMR and evaluated for α-glucosidase inhibitory potential. All twenty one derivatives showed good α-glucosidase inhibitory activity with IC50 value ranging between 18.23 ± 0.03 and 424.41 ± 0.94 μM when compared with t...

Full description

Bibliographic Details
Published in:Bioorganic Chemistry
Main Author: Rahim F.; Ullah H.; Javid M.T.; Wadood A.; Taha M.; Ashraf M.; Shaukat A.; Junaid M.; Hussain S.; Rehman W.; Mehmood R.; Sajid M.; Khan M.N.; Khan K.M.
Format: Article
Language:English
Published: Academic Press Inc. 2015
Online Access:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84935492350&doi=10.1016%2fj.bioorg.2015.06.006&partnerID=40&md5=28062b694b741d707e1fda11bd617d5d
id 2-s2.0-84935492350
spelling 2-s2.0-84935492350
Rahim F.; Ullah H.; Javid M.T.; Wadood A.; Taha M.; Ashraf M.; Shaukat A.; Junaid M.; Hussain S.; Rehman W.; Mehmood R.; Sajid M.; Khan M.N.; Khan K.M.
Synthesis, in vitro evaluation and molecular docking studies of thiazole derivatives as new inhibitors of α-glucosidase
2015
Bioorganic Chemistry
62

10.1016/j.bioorg.2015.06.006
https://www.scopus.com/inward/record.uri?eid=2-s2.0-84935492350&doi=10.1016%2fj.bioorg.2015.06.006&partnerID=40&md5=28062b694b741d707e1fda11bd617d5d
A series of thiazole derivatives 1-21 were prepared, characterized by EI-MS and 1H NMR and evaluated for α-glucosidase inhibitory potential. All twenty one derivatives showed good α-glucosidase inhibitory activity with IC50 value ranging between 18.23 ± 0.03 and 424.41 ± 0.94 μM when compared with the standard acarbose (IC50, 38.25 ± 0.12 μM). Compound (8) (IC50, 18.23 ± 0.03 μM) and compound (7) (IC50 = 36.75 ± 0.05 μM) exhibited outstanding inhibitory potential much better than the standard acarbose (IC50, 38.25 ± 0.12 μM). All other analogs also showed good to moderate enzyme inhibition. Molecular docking studies were carried out in order to find the binding affinity of thiazole derivatives with enzyme. Studies showed these thiazole analogs as a new class of α-glucosidase inhibitors. © 2015 Published by Elsevier Inc.
Academic Press Inc.
452068
English
Article
author Rahim F.; Ullah H.; Javid M.T.; Wadood A.; Taha M.; Ashraf M.; Shaukat A.; Junaid M.; Hussain S.; Rehman W.; Mehmood R.; Sajid M.; Khan M.N.; Khan K.M.
spellingShingle Rahim F.; Ullah H.; Javid M.T.; Wadood A.; Taha M.; Ashraf M.; Shaukat A.; Junaid M.; Hussain S.; Rehman W.; Mehmood R.; Sajid M.; Khan M.N.; Khan K.M.
Synthesis, in vitro evaluation and molecular docking studies of thiazole derivatives as new inhibitors of α-glucosidase
author_facet Rahim F.; Ullah H.; Javid M.T.; Wadood A.; Taha M.; Ashraf M.; Shaukat A.; Junaid M.; Hussain S.; Rehman W.; Mehmood R.; Sajid M.; Khan M.N.; Khan K.M.
author_sort Rahim F.; Ullah H.; Javid M.T.; Wadood A.; Taha M.; Ashraf M.; Shaukat A.; Junaid M.; Hussain S.; Rehman W.; Mehmood R.; Sajid M.; Khan M.N.; Khan K.M.
title Synthesis, in vitro evaluation and molecular docking studies of thiazole derivatives as new inhibitors of α-glucosidase
title_short Synthesis, in vitro evaluation and molecular docking studies of thiazole derivatives as new inhibitors of α-glucosidase
title_full Synthesis, in vitro evaluation and molecular docking studies of thiazole derivatives as new inhibitors of α-glucosidase
title_fullStr Synthesis, in vitro evaluation and molecular docking studies of thiazole derivatives as new inhibitors of α-glucosidase
title_full_unstemmed Synthesis, in vitro evaluation and molecular docking studies of thiazole derivatives as new inhibitors of α-glucosidase
title_sort Synthesis, in vitro evaluation and molecular docking studies of thiazole derivatives as new inhibitors of α-glucosidase
publishDate 2015
container_title Bioorganic Chemistry
container_volume 62
container_issue
doi_str_mv 10.1016/j.bioorg.2015.06.006
url https://www.scopus.com/inward/record.uri?eid=2-s2.0-84935492350&doi=10.1016%2fj.bioorg.2015.06.006&partnerID=40&md5=28062b694b741d707e1fda11bd617d5d
description A series of thiazole derivatives 1-21 were prepared, characterized by EI-MS and 1H NMR and evaluated for α-glucosidase inhibitory potential. All twenty one derivatives showed good α-glucosidase inhibitory activity with IC50 value ranging between 18.23 ± 0.03 and 424.41 ± 0.94 μM when compared with the standard acarbose (IC50, 38.25 ± 0.12 μM). Compound (8) (IC50, 18.23 ± 0.03 μM) and compound (7) (IC50 = 36.75 ± 0.05 μM) exhibited outstanding inhibitory potential much better than the standard acarbose (IC50, 38.25 ± 0.12 μM). All other analogs also showed good to moderate enzyme inhibition. Molecular docking studies were carried out in order to find the binding affinity of thiazole derivatives with enzyme. Studies showed these thiazole analogs as a new class of α-glucosidase inhibitors. © 2015 Published by Elsevier Inc.
publisher Academic Press Inc.
issn 452068
language English
format Article
accesstype
record_format scopus
collection Scopus
_version_ 1809678486938320896

Similar Items