Issue 8, 2017

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

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

Supplementary files

Article information

Article type
Research Article
Submitted
03 Apr 2017
Accepted
08 Jun 2017
First published
14 Jun 2017

Med. Chem. Commun., 2017,8, 1618-1630

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, 8, 1618 DOI: 10.1039/C7MD00162B

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