Synthesis, α-glucosidase inhibition and molecular docking study of coumarin based derivatives

Bioorganic Chemistry
Muhammad TahaKhalid Mohammed Khan

Abstract

We have synthesized seventeen Coumarin based derivatives (1-17), characterized by 1HNMR, 13CNMR and EI-MS and evaluated for α-glucosidase inhibitory potential. Among the series, all derivatives exhibited outstanding α-glucosidase inhibition with IC50 values ranging between 1.10 ± 0.01 and 36.46 ± 0.70 μM when compared with the standard inhibitor acarbose having IC50 value 39.45 ± 0.10 μM. The most potent derivative among the series is derivative 3 having IC50 value 1.10 ± 0.01 μM, which are many folds better than the standard acarbose. The structure activity relationship (SAR) was mainly based upon by bring about difference of substituent's on phenyl part. Molecular docking studies were carried out to understand the binding interaction of the most active compounds.

Citations

Sep 29, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Md ShahinozzamanShinkichi Tawata
Oct 31, 2018·Archiv der Pharmazie·Emre MenteşeMustafa Emirik
Mar 29, 2019·Protein and Peptide Letters·Sameer Suresh BhagyawantNidhi Srivastava
Sep 26, 2019·Mini Reviews in Medicinal Chemistry·Tadesse Bekele TafesseMohsen Amini

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