Triazinoindole analogs as potent inhibitors of α-glucosidase: Synthesis, biological evaluation and molecular docking studies

Triazinoindole analogs as potent inhibitors of α-glucosidase: Synthesis, biological evaluation and molecular docking studies

A new series of triazinoindole analogs 1-11 were synthesized, characterized by EI-MS and 1H NMR, evaluated for α-glucosidase inhibitory potential. All eleven (11) analogs showed different range of α-glucosidase inhibitory potential with IC50 value ranging between 2.46 ± 0.008 and 312.79 ± 0.06 μM wh...

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Published in:Bioorganic Chemistry
Main Author: Rahim F.; Ullah K.; Ullah H.; Wadood A.; Taha M.; Rehman A.U.; Uddin I.; Ashraf M.; Shaukat A.; Rehman W.; Hussain S.; Khan K.M.
Format: Article
Language:English
Published: Academic Press Inc. 2015
Online Access:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84919941245&doi=10.1016%2fj.bioorg.2014.12.001&partnerID=40&md5=79a338ff4fb9911bebc292bf68f10017
id 2-s2.0-84919941245
spelling 2-s2.0-84919941245
Rahim F.; Ullah K.; Ullah H.; Wadood A.; Taha M.; Rehman A.U.; Uddin I.; Ashraf M.; Shaukat A.; Rehman W.; Hussain S.; Khan K.M.
Triazinoindole analogs as potent inhibitors of α-glucosidase: Synthesis, biological evaluation and molecular docking studies
2015
Bioorganic Chemistry
58

10.1016/j.bioorg.2014.12.001
https://www.scopus.com/inward/record.uri?eid=2-s2.0-84919941245&doi=10.1016%2fj.bioorg.2014.12.001&partnerID=40&md5=79a338ff4fb9911bebc292bf68f10017
A new series of triazinoindole analogs 1-11 were synthesized, characterized by EI-MS and 1H NMR, evaluated for α-glucosidase inhibitory potential. All eleven (11) analogs showed different range of α-glucosidase inhibitory potential with IC50 value ranging between 2.46 ± 0.008 and 312.79 ± 0.06 μM when compared with the standard acarbose (IC50, 38.25 ± 0.12 μM). Among the series, compounds 1, 3, 4, 5, 7, 8, and 11 showed excellent inhibitory potential with IC50 values 2.46 ± 0.008, 37.78 ± 0.05, 28.91 ± 0.0, 38.12 ± 0.04, 37.43 ± 0.03, 36.89 ± 0.06 and 37.11 ± 0.05 μM respectively. All other compounds also showed good enzyme inhibition. The binding modes of these analogs were confirmed through molecular docking. © 2014 Elsevier B.V. All rights reserved.
Academic Press Inc.
452068
English
Article
author Rahim F.; Ullah K.; Ullah H.; Wadood A.; Taha M.; Rehman A.U.; Uddin I.; Ashraf M.; Shaukat A.; Rehman W.; Hussain S.; Khan K.M.
spellingShingle Rahim F.; Ullah K.; Ullah H.; Wadood A.; Taha M.; Rehman A.U.; Uddin I.; Ashraf M.; Shaukat A.; Rehman W.; Hussain S.; Khan K.M.
Triazinoindole analogs as potent inhibitors of α-glucosidase: Synthesis, biological evaluation and molecular docking studies
author_facet Rahim F.; Ullah K.; Ullah H.; Wadood A.; Taha M.; Rehman A.U.; Uddin I.; Ashraf M.; Shaukat A.; Rehman W.; Hussain S.; Khan K.M.
author_sort Rahim F.; Ullah K.; Ullah H.; Wadood A.; Taha M.; Rehman A.U.; Uddin I.; Ashraf M.; Shaukat A.; Rehman W.; Hussain S.; Khan K.M.
title Triazinoindole analogs as potent inhibitors of α-glucosidase: Synthesis, biological evaluation and molecular docking studies
title_short Triazinoindole analogs as potent inhibitors of α-glucosidase: Synthesis, biological evaluation and molecular docking studies
title_full Triazinoindole analogs as potent inhibitors of α-glucosidase: Synthesis, biological evaluation and molecular docking studies
title_fullStr Triazinoindole analogs as potent inhibitors of α-glucosidase: Synthesis, biological evaluation and molecular docking studies
title_full_unstemmed Triazinoindole analogs as potent inhibitors of α-glucosidase: Synthesis, biological evaluation and molecular docking studies
title_sort Triazinoindole analogs as potent inhibitors of α-glucosidase: Synthesis, biological evaluation and molecular docking studies
publishDate 2015
container_title Bioorganic Chemistry
container_volume 58
container_issue
doi_str_mv 10.1016/j.bioorg.2014.12.001
url https://www.scopus.com/inward/record.uri?eid=2-s2.0-84919941245&doi=10.1016%2fj.bioorg.2014.12.001&partnerID=40&md5=79a338ff4fb9911bebc292bf68f10017
description A new series of triazinoindole analogs 1-11 were synthesized, characterized by EI-MS and 1H NMR, evaluated for α-glucosidase inhibitory potential. All eleven (11) analogs showed different range of α-glucosidase inhibitory potential with IC50 value ranging between 2.46 ± 0.008 and 312.79 ± 0.06 μM when compared with the standard acarbose (IC50, 38.25 ± 0.12 μM). Among the series, compounds 1, 3, 4, 5, 7, 8, and 11 showed excellent inhibitory potential with IC50 values 2.46 ± 0.008, 37.78 ± 0.05, 28.91 ± 0.0, 38.12 ± 0.04, 37.43 ± 0.03, 36.89 ± 0.06 and 37.11 ± 0.05 μM respectively. All other compounds also showed good enzyme inhibition. The binding modes of these analogs were confirmed through molecular docking. © 2014 Elsevier B.V. All rights reserved.
publisher Academic Press Inc.
issn 452068
language English
format Article
accesstype
record_format scopus
collection Scopus
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