2-Aryl benzimidazoles: Synthesis, In vitro alpha-amylase inhibitory activity, and molecular docking study
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Date
2018-03-06
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Publisher
Elsevier
Abstract
Despite of many diverse biological activities exhibited by benzimidazole scaffold, it is rarely explored for
the -amylase inhibitory activity. For that purpose, 2-aryl benzimidazole derivatives 1-45 were synthesized
and screened for in vitro -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 M, when compared to the standard acarbose
(IC50 = 1.46 ± 0.26 M). 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 -amylase enzyme, in silico study was
conducted.
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Keywords
Benzimidazole, alpha-Amylase, In vitro, In silico, Structure-activity relationship (SAR)