Randomized trial evaluates anti-diabetic efficacy of novel compounds in targeting enzymes, suggesting further development.
Key Points
This work aims to synthesize and evaluate the efficacy of pyrimidine-derived pyrazole-thiadiazole derivatives in inhibiting key enzymes related to diabetes mellitus.
Synthesis and characterization of novel thiadiazole derivatives aimed at inhibiting α-amylase and α-glucosidase.
Evaluation of inhibitory activity through IC50 determination compared to Acarbose.
Molecular docking analysis to assess binding interactions and DFT calculations for electronic properties.
All synthesized derivatives, except three, inhibited α-amylase with IC50 values ranging from 5.17 μM to 29.84 μM.
Inhibition of α-glucosidase by derivatives had IC50 values from 7.60 μM to 31.62 μM.
Analogs 8g, 8k, and 8b demonstrated superior or comparable activity to Acarbose, indicating potential for further drug development.