A novel series of chromone-isatin derivatives 6a-6p were designed, synthesized and characterized by H NMR, C NMR and HRMS. These novel synthetic compounds were evaluated for inhibitory activity against yeast α-glucosidase enzyme. The results of biological test have shown that all tested compounds exhibited excellent to potent inhibitory activity in the range of IC = 3.18 ± 0.12-16.59 ± 0.17 μM as compared to the standard drug acarbose (IC = 817.38 ± 6.27 μM). Compound 6j (IC = 3.18 ± 0.12 μM) with a hydroxyl group at the 7-position of chromone and a 4-bromobenzyl group at the N1-positions of isatin, was found to be the most active compound among the series. Furthermore, molecular docking study was performed to help understand binding interactions of the most active analogs with α-glucosidase enzyme. These results indicated that this class of compounds had potential for the development of anti-diabetic agents.
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| http://dx.doi.org/10.1016/j.bmcl.2017.11.047 | DOI Listing |
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