SYNTHESIS, PHARMACOLOGICAL EVALUATION AND LIGAND-PROTEIN INTERACTION STUDY OF HYBRID UREA AND THIOUREA DERIVATIVES AS ANTIHYPERGLYCEMIC AGENTS

Abstract

The study focuses on the synthesis and pharmacological evaluation of hybrid urea and thiourea derivatives with a chalcone moiety, aimed at treating type-II diabetes.

• Methods:

  • Synthesis of the derivatives (5a-5f).

  • In vitro α-glucosidase inhibition assay.

  • In vivo antidiabetic activity in a streptozotocin (STZ)-induced diabetic rat model.

  • Molecular docking studies to understand ligand-protein interactions.

• Results:

  • Compound 5d demonstrated the most potency with an IC50 value of 12.88 µM compared to the standard drug Acarbose (IC50 16.54 µM).

  • In vivo studies showed that compound 5d was more effective in managing diabetes compared to other synthesized molecules.

  • Molecular docking confirmed effective interactions with the target protein.

• Conclusion:

  • The hybrid urea/thiourea derivatives, particularly compound 5d, are promising candidates for further development as antidiabetic agents.