Benzimidazole derivatives as new α-glucosidase inhibitors and in silico studies

Benzimidazole derivatives as new α-glucosidase inhibitors and in silico studies

Newly synthesized benzimidazole hydrazone derivatives 1-26 were evaluated for their α-glucosidase inhibitory activity. Compounds 1-26 exhibited varying degrees of yeast α-glucosidase inhibitory activity with IC50 values between 8.40 ± 0.76 and 179.71 ± 1.11 μM when compared with standard acarbose. I...

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Published in:Bioorganic Chemistry
Main Author: Zawawi N.K.N.A.; Taha M.; Ahmat N.; Wadood A.; Ismail N.H.; Rahim F.; Azam S.S.; Abdullah N.
Format: Article
Language:English
Published: Academic Press Inc. 2016
Online Access:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84948649641&doi=10.1016%2fj.bioorg.2015.11.006&partnerID=40&md5=93ec464c2d71e54bbd8588cac5d567e0
id 2-s2.0-84948649641
spelling 2-s2.0-84948649641
Zawawi N.K.N.A.; Taha M.; Ahmat N.; Wadood A.; Ismail N.H.; Rahim F.; Azam S.S.; Abdullah N.
Benzimidazole derivatives as new α-glucosidase inhibitors and in silico studies
2016
Bioorganic Chemistry
64

10.1016/j.bioorg.2015.11.006
https://www.scopus.com/inward/record.uri?eid=2-s2.0-84948649641&doi=10.1016%2fj.bioorg.2015.11.006&partnerID=40&md5=93ec464c2d71e54bbd8588cac5d567e0
Newly synthesized benzimidazole hydrazone derivatives 1-26 were evaluated for their α-glucosidase inhibitory activity. Compounds 1-26 exhibited varying degrees of yeast α-glucosidase inhibitory activity with IC50 values between 8.40 ± 0.76 and 179.71 ± 1.11 μM when compared with standard acarbose. In this assay, seven compounds that showed highest inhibitory effects than the rest of benzimidazole series were identified. All the synthesized compounds were characterized by different spectroscopic methods adequately. We further evaluated the interaction of the active compounds with enzyme with the help of docking studies. © 2015 Elsevier Inc. All rights reserved.
Academic Press Inc.
452068
English
Article
author Zawawi N.K.N.A.; Taha M.; Ahmat N.; Wadood A.; Ismail N.H.; Rahim F.; Azam S.S.; Abdullah N.
spellingShingle Zawawi N.K.N.A.; Taha M.; Ahmat N.; Wadood A.; Ismail N.H.; Rahim F.; Azam S.S.; Abdullah N.
Benzimidazole derivatives as new α-glucosidase inhibitors and in silico studies
author_facet Zawawi N.K.N.A.; Taha M.; Ahmat N.; Wadood A.; Ismail N.H.; Rahim F.; Azam S.S.; Abdullah N.
author_sort Zawawi N.K.N.A.; Taha M.; Ahmat N.; Wadood A.; Ismail N.H.; Rahim F.; Azam S.S.; Abdullah N.
title Benzimidazole derivatives as new α-glucosidase inhibitors and in silico studies
title_short Benzimidazole derivatives as new α-glucosidase inhibitors and in silico studies
title_full Benzimidazole derivatives as new α-glucosidase inhibitors and in silico studies
title_fullStr Benzimidazole derivatives as new α-glucosidase inhibitors and in silico studies
title_full_unstemmed Benzimidazole derivatives as new α-glucosidase inhibitors and in silico studies
title_sort Benzimidazole derivatives as new α-glucosidase inhibitors and in silico studies
publishDate 2016
container_title Bioorganic Chemistry
container_volume 64
container_issue
doi_str_mv 10.1016/j.bioorg.2015.11.006
url https://www.scopus.com/inward/record.uri?eid=2-s2.0-84948649641&doi=10.1016%2fj.bioorg.2015.11.006&partnerID=40&md5=93ec464c2d71e54bbd8588cac5d567e0
description Newly synthesized benzimidazole hydrazone derivatives 1-26 were evaluated for their α-glucosidase inhibitory activity. Compounds 1-26 exhibited varying degrees of yeast α-glucosidase inhibitory activity with IC50 values between 8.40 ± 0.76 and 179.71 ± 1.11 μM when compared with standard acarbose. In this assay, seven compounds that showed highest inhibitory effects than the rest of benzimidazole series were identified. All the synthesized compounds were characterized by different spectroscopic methods adequately. We further evaluated the interaction of the active compounds with enzyme with the help of docking studies. © 2015 Elsevier Inc. All rights reserved.
publisher Academic Press Inc.
issn 452068
language English
format Article
accesstype
record_format scopus
collection Scopus
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