Jump to main content
Jump to site search
PLANNED MAINTENANCE Close the message box

Scheduled maintenance work on Wednesday 27th March 2019 from 11:00 AM to 1:00 PM (GMT).

During this time our website performance may be temporarily affected. We apologise for any inconvenience this might cause and thank you for your patience.


Issue 21, 2018
Previous Article Next Article

Design, synthesis and in vitro α-glucosidase inhibition of novel coumarin-pyridines as potent antidiabetic agents

Author affiliations

Abstract

In this work, we report an efficient, one-pot and three-component synthesis of novel coumarin fused pyridine derivatives 4a–p. Heating the mixture of 4-hydroxycoumarins and ammonium acetate in DMF gave the corresponding 4-aminocoumarins, which subsequently went through Michael addition–cyclocondensation with α-azidochalcone derivatives to produce our desired products in high yields. The synthesized compounds 4a–p were evaluated for α-glucosidase inhibitory activity and all of them exhibited excellent in vitro yeast α-glucosidase inhibition with IC50 values ranging from 101.0 ± 2.0 to 227.3 ± 1.4 μM when compared with the standard drug acarbose (IC50 = 750.0 ± 1.5 μM). A kinetic study of the most potent compound 4i revealed that it inhibited α-glucosidase in a competitive mode. A docking study of the most active compounds 4i, 4h, and 4j was also performed.

Graphical abstract: Design, synthesis and in vitro α-glucosidase inhibition of novel coumarin-pyridines as potent antidiabetic agents

Back to tab navigation

Supplementary files

Publication details

The article was received on 20 May 2018, accepted on 17 Sep 2018 and first published on 18 Sep 2018


Article type: Paper
DOI: 10.1039/C8NJ02495B
Citation: New J. Chem., 2018,42, 17268-17278

  •   Request permissions

    Design, synthesis and in vitro α-glucosidase inhibition of novel coumarin-pyridines as potent antidiabetic agents

    M. Adib, F. Peytam, M. Rahmanian-Jazi, M. Mohammadi-Khanaposhtani, S. Mahernia, H. R. Bijanzadeh, M. Jahani, S. Imanparast, M. A. Faramarzi, M. Mahdavi and B. Larijani, New J. Chem., 2018, 42, 17268
    DOI: 10.1039/C8NJ02495B

Search articles by author

Spotlight

Advertisements