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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Bibliographic Details
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
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Summary: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.
ISSN:452068
DOI:10.1016/j.bioorg.2015.11.006