Journal article
2-Aryl benzimidazoles

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Publication Details
Subtitle: Synthesis, In vitro α-amylase inhibitory activity, and molecular docking study
Author list: Akande Akinsola Adegboye, Khalid Mohammed Khan, Uzma Salar, Sherifat Adeyinka Aboaba, Kanwal, Sridevi Chigurupati, Itrat Fatima, Mohammad Taha, Abdul Wadood, Jahidul Isalm Mohammad, Huma Khan, Shahnaz Perveen
Publisher: Elsevier
Publication year: 2018
Journal: European Journal of Medicinal Chemistry
Volume number: 150
Issue number: 25 April 2018
Start page: 248
End page: 260
Number of pages: 13
ISSN: 0223-5234
Web of Science ID: 000430891400018
PubMed ID: 29533872
Scopus ID: 85043359288

Despite of many diverse biological activities exhibited by benzimidazole scaffold,
it is rarely explored for the α-amylase inhibitory activity. For that purpose, 2-aryl
benzimidazole derivatives 1-45 were synthesized and screened for in vitro α-amylase
inhibitory activity. Structures of all synthetic compounds were deduced by various
spectroscopic techniques. All compounds revealed inhibition potential with IC50 values of
1.48 ± 0.38-2.99 ± 0.14 μM, when compared to the standard acarbose (IC50 = 1.46 ± 0.26
μM). Limited SAR suggested that the variation in the inhibitory activities of the compounds
are the result of different substitutions on aryl ring. In order to rationalize the binding
interactions of most active compounds with the active site of α-amylase enzyme, in silico
study was conducted.

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Last updated on 2019-03-04 at 13:16