Chalcones and bis-chalcones: As potential α-amylase inhibitors; synthesis, in vitro screening, and molecular modelling studies

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dc.contributor.authorBale, Adebayo Tajudeen
dc.contributor.authorKhan, Khalid Mohammed
dc.contributor.authorSalar, Uzma
dc.contributor.authorChigurupati, Sridevi
dc.contributor.authorFasina, Tolulope
dc.contributor.authorAli, Farman
dc.contributor.authorKanwal
dc.contributor.authorAbdul Wadood
dc.contributor.authorTaha, Muhammad
dc.contributor.authorNanda, Sekhar Sitanshu
dc.contributor.authorGhufran Mehreen
dc.contributor.authorPerveen, Shahnaz
dc.date.accessioned2024-08-12T17:51:42Z
dc.date.available2024-08-12T17:51:42Z
dc.date.issued2018-05-07
dc.description.abstractDespite of a diverse range of biological activities associated with chalcones and bis-chalcones, they are still neglected by the medicinal chemist for their possible α-amylase inhibitory activity. So, the current study is based on the evaluation of this class for the identification of new leads as α-amylase inhibitors. For that purpose, a library of substituted chalcones 1–13 and bis-chalcones 14–18 were synthesized and characterized by spectroscopic techniques EI-MS and 1H NMR. CHN analysis was carried out and found in agreement with the calculated values. All compounds were evaluated for in vitro α-amylase inhibitory activity and demonstrated good activities in the range of IC50 = 1.25 ± 1.05–2.40 ± 0.09 µM as compared to the standard acarbose (IC50 = 1.04 ± 0.3 µM). Limited structure–activity relationship (SAR) was established by considering the effect of different groups attached to aryl rings on varying inhibitory activity. SMe group in chalcones and OMe group in bis-chalcones were found more influential on the activity than other groups. However, in order to predict the involvement of different groups in the binding interactions with the active site of α-amylase enzyme, in silico studies were also conducted.
dc.identifier.urihttps://kwasuspace.kwasu.edu.ng/handle/123456789/2268
dc.publisherAcademic Press Inc.
dc.titleChalcones and bis-chalcones: As potential α-amylase inhibitors; synthesis, in vitro screening, and molecular modelling studies
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