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Bioorg Chem. 2017 Aug;73:1-9. doi: 10.1016/j.bioorg.2017.05.009. Epub 2017 May 10.

Hetarylcoumarins: Synthesis and biological evaluation as potent α-glucosidase inhibitors.

Author information

1
Department of Chemistry, Kinnaird College for Women, Lahore 54000, Pakistan. Electronic address: frylchaudhry@yahoo.com.
2
Department of Biotechnology, Kinnaird College for Women, Lahore 54000, Pakistan.
3
Department of Chemistry, Kinnaird College for Women, Lahore 54000, Pakistan.
4
Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.
5
Department of Chemistry, Forman Christian College (A Chartered University), Ferozepur Road, Lahore 54600, Pakistan.
6
Institute of Chemistry, University of the Punjab, Lahore 54590, Pakistan. Electronic address: mamunawar.chem@pu.edu.pk.
7
Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan; Institute of Chemistry, University of the Punjab, Lahore 54590, Pakistan.

Abstract

In search of better α-glucosidase inhibitors, a series of novel hetarylcoumarins (3a-3j) were designed and synthesized through a facile multicomponent route where p-toluenesulfonic acid (PTSA) was explored as an efficient catalyst. These new scaffolds were further evaluated for their α-glucosidase inhibition potentials. All the derivatives exhibited good to excellent results which were comparable or even better than of standard drug acarbose. Of these compounds, a dihalogenated compound 3f was found to be the most effective one with IC50: 2.53±0.002µM. Molecular docking has predicted the plausible binding interactions of compounds 3f, 3g and 3j with α-glucosidase.

KEYWORDS:

Antidiabetic agents; Coumarin; Imidazole; Molecular docking; α-Glucosidase inhibitors

PMID:
28521172
DOI:
10.1016/j.bioorg.2017.05.009
[Indexed for MEDLINE]

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