Synthesis of Cyclopyrrolidine Clubbed with Oxadiazole Bases and Evaluation of their Anti-Diabetic Activity through in vivo Model

Abstract:

Background and Aim: Based on inhibitors of DPP-IV, there is a fantastic method for creating anti-diabetic medications. These inhibitors regulate diabetic patients' blood sugar levels to prevent difficulties with their health. In the current work, we created a brand-new series of compounds Cyclopyrrolidine clubbed with oxadiazole bases. Materials and Methods: Cyclopyrrolidine clubbed with oxadiazole bases (B-1 to B-16) were synthesized and characterized through IR, NMR, mass spectrometry, and elemental analysis. Docking studies were performed to assess interactions and binding modes of synthesized hits at the binding site of receptor DPP-4 (PDB 3W2T). Using vildagliptin as a standard drug, six of the synthesized compounds were tested for their antidiabetic activity in diabetic rats induced with HFD-STZ-Nicotinamide. Results: The results showed that compound B-XIV (220*4.56B) resulted in the greatest reduction in blood glucose level from all synthesized compounds compared to that of vildagliptin (215*7.52B) in HFD-STZ-Nicotinamide. Other compounds showed moderate to good antihyperglycemic activity. Conclusion: From he presents work it can be concluded that synthesized compounds possess good DPP-IV inhibitory activity. Compounds containing electron-withdrawing groups (chlorine, nitro, methoxy) were displayed a good anti-diabetic effect than electron-donating groups (methyl, hydroxyl). Oxadiazole derivatives could be used for further development to obtain more promising drug candidates.

Keywords: Furadiazole, Hyperglycaemic, HFD-STZ-Nicotinamide.