A series of novel isatin-thiazole derivatives were synthesized and screened for their in vitro α-glucosidase inhibitory activity. These compounds displayed a varying degree of α-glucosidase inhibitory activity with IC ranging from 5.36 ± 0.13 to 35.76 ± 0.31 μm as compared to the standard drug acarbose (IC = 817.38 ± 6.27 μm). Among the series, compound bearing a hydroxyl group at the 4-position of the right phenyl and 2-fluorobenzyl substituent at the 1-positions of the 5-methylisatin displayed the highest inhibitory activity with an IC value of 5.36 ± 0.13 μm. Molecular docking studies revealed the existence of hydrophobic interaction, CH-π interaction, arene-anion interaction, arene-cation interaction, and hydrogen bond between these compounds and α-glucosidase enzyme.
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| http://dx.doi.org/10.3390/molecules22040659 | DOI Listing |
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