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Chem Biol Drug Des. 2017 Mar;89(3):456-463. doi: 10.1111/cbdd.12867. Epub 2016 Oct 5.

Synthesis, in vitro evaluation and molecular docking studies of novel coumarin-isatin derivatives as α-glucosidase inhibitors.

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College of Chemistry and Chemical Engineering, Jishou University, Jishou, China.


This study synthesized a series of novel coumarin-isatin derivatives and evaluated them for α-glucosidase inhibitory activity. The majority of the screened compounds exhibited excellent inhibition activities with IC50 values of 2.56 ± 0.08-268.79 ± 3.04 μm, when compared to acarbose. Among the newly derivatives, compound 5p was found to be the most active compound in the library of coumarin-isatin derivatives. Furthermore, enzyme kinetic studies showed that compound 5p is a non-competitive inhibitor with a Ki of 2.14 μm. Molecular docking analysis revealed the existence of hydrophobic and hydrogen interactions between compound 5p and the active site of α-glucosidase. Our results indicate that coumarin-isatin derivatives as a new class of α-glucosidase inhibitors.


coumarin; enzyme kinetic study; isatin; molecular docking; α-glucosidase inhibitor

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