Thiazolidinedione-triazole conjugates: design, synthesis and probing of the α-amylase inhibitory potential.

Aim: The primary objective of this investigation was the synthesis, spectral interpretation and evaluation of the α-amylase inhibition of rationally designed thiazolidinedione-triazole conjugates ( 7a-7aa ). Materials & methods: The designed compounds were synthesized by stirring a mixture of thiazolidine-2,4-dione, propargyl bromide, cinnamaldehyde and azide derivatives in polyethylene glycol-400. The α-amylase inhibitory activity of the synthesized conjugates was examined by integrating in vitro and in silico studies. Results: The investigated derivatives exhibited promising α-amylase inhibitory activity, with IC ₅₀ values ranging between 0.028 and 0.088 μmol ml ^-1 . Various computational approaches were employed to get detailed information about the inhibition mechanism. Conclusion: The thiazolidinedione-triazole conjugate 7p , with IC ₅₀  = 0.028 μmol ml ^-1 , was identified as the best hit for inhibiting α-amylase.