| Summary: | A series of thiazole-based thiazolidinone derivatives (1-20) have been synthesized and evaluated against α-glucosidase and α-amylase enzymes. All derivatives showed good α-glucosidase activity having IC50 values ranging from 2.40 ± 0.10 to 31.40 ± 0.90 μM and for α-amylase having IC50 values ranging from 1.80 ± 0.05 to 27.60 ± 0.80 μM as compared to standard drug acarbose (IC50 = 9.80 ± 0.20 μM & 10.30 ±0.20 μM respectively). Analogues 5 (IC50 = 1.80 ± 0.05 & 2.40 ± 0.10 µM) and 10 (IC50 = 2.10 ± 0.10 & 3.60 ± 0.20 µM) showed potent inhibitory potential against both alpha-glucosidase and alpha-amylase enzymes. The structure-activity relationship has been established which mainly depends upon the number, nature, position, and electron donating/withdrawing effect of substituent/s on the aryl ring. A molecular docking study was also carried out to determine the binding interactions of the most potent analogues with the active site of the enzyme. © 2022 Elsevier B.V.
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