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Synthesis, molecular modeling and biological evaluation of aza-flavanones as α-glucosidase inhibitors

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Abstract

An efficient acid catalyzed methodology has been employed to synthesize a variety of aza-flavanones and their α-glucosidase inhibitory activity is evaluated using acarbose, miglitol and voglibose as reference standards. Molecular modeling studies were performed for all compounds to identify the important binding modes responsible for the inhibition activity of α-glucosidase which helped find key interactions between the enzyme and the active compounds. Among all the compounds 5g, 5r and 5w have shown high α-glucosidase inhibition activity compared to standard reference drugs and have been identified as promising potential antidiabetic agents. This study is the first biological evaluation of aza-flavanones as α-glucosidase inhibitors.

Graphical abstract: Synthesis, molecular modeling and biological evaluation of aza-flavanones as α-glucosidase inhibitors

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Publication details

The article was received on 03 Apr 2017, accepted on 08 Jun 2017 and first published on 14 Jun 2017


Article type: Research Article
DOI: 10.1039/C7MD00162B
Citation: Med. Chem. Commun., 2017, Advance Article
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    Synthesis, molecular modeling and biological evaluation of aza-flavanones as α-glucosidase inhibitors

    S. Kasturi, S. Surarapu, C. C. Bathoju, S. Uppalanchi, S. Dwivedi, Y. Perumal, D. K. Sigalapalli, B. N. Babu, K. S. Ethiraj and J. S. Anireddy, Med. Chem. Commun., 2017, Advance Article , DOI: 10.1039/C7MD00162B

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