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

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dc.contributor.authorBale, A.T.
dc.contributor.authorKhan, K.M.
dc.contributor.authorSalar, U.
dc.contributor.authorChigurupati, S.
dc.contributor.authorFasina, T.M.
dc.contributor.authorAli, F.
dc.contributor.authorKanwal
dc.contributor.authorWadood, A.
dc.contributor.authorTaha, M.
dc.contributor.authorNanda, S.S.
dc.contributor.authorGhufran, M.
dc.contributor.authorPerveen, S.
dc.date.accessioned2019-09-06T07:59:58Z
dc.date.available2019-09-06T07:59:58Z
dc.date.issued2018-05-07
dc.descriptionStaff publicationsen_US
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.en_US
dc.identifier.citationBale, A. T., [Et...al] (2018). Chalcones and bis-chalcones: As potential α-amylase inhibitors; synthesis, in vitro screening, and molecular modelling studies. Bioorganic chemistry, Vol.79, 179-189pp.en_US
dc.identifier.urihttps://ir.unilag.edu.ng/handle/123456789/5367
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.relation.ispartofseriesBioorganic chemistry;Vol.79
dc.subjectResearch Subject Categories::NATURAL SCIENCES::Chemistry::Organic chemistry::Bioorganic chemistryen_US
dc.subjectChalconesen_US
dc.subjectBis-chalconesen_US
dc.subjectIn vitroen_US
dc.subjectα-amylaseen_US
dc.subjectinhibitory activityen_US
dc.subjectStructure-activity relationshipen_US
dc.titleChalcones and bis-chalcones: As potential α-amylase inhibitors; synthesis, in vitro screening, and molecular modelling studiesen_US
dc.typeArticleen_US
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