Synthesis, Characterization, and Evaluation of in vitro Antidiabetic Activity of Novel Pyrrolidine Sulphonamide Derivative

  • Megha Tukaram Salve Department of Pharmaceutical Chemistry, Modern College of Pharmacy, Nigdi, Pune, Maharashtra, INDIA.
  • Shailaja Bhanudas Jadhav Department of Pharmaceutical Chemistry, Modern College of Pharmacy, Nigdi, Pune, Maharashtra, INDIA.
Keywords: Pyrrolidine sulphonamide derivative, 1,2,4-oxadiazole, In vitro study, Antidiabetic, Dipeptidyl peptidase-4

Abstract

Background: Diabetes is a long-term illness characterized by high blood sugar levels. It is estimated that by 2045, there will be nearly 693 million diabetic patients worldwide, with half of the population remaining undiagnosed. Metformin, insulin, sulfonylureas, and thiazolidinediones were related to several risk factors, including hypoglycemia, bone fracture, weight gain, cardiovascular, renal, and other complications. In the present study, we have explored the DPP-IV inhibitors as a new class of antidiabetic drugs. Objectives: The goal of DPP-IV inhibitors is to raise levels of incretins (GLP-1 and GIP), which block glucagon release while boosting insulin secretion, slowing stomach emptying, and reducing blood glucose levels. Methods: A series of derivatives substituted on Oxadiazole of sulfonamide pyrrolidine were produced by reacting 1,2,4-oxadiazol and sulfonyl chloride at room temperature in the presence of ethanol and stirring until the reaction was complete. The compounds were characterized using IR, 1H NMR, C13 NMR, mass spectroscopy, elemental analysis, and screened for in vitro assay of DPP-IV inhibition. Results and Discussion: The IC50 was calculated for compounds B-I, B-V, B-VI, B-XI, and B-XIII that inhibited enzymes significantly, IC50 values ranging from 19.65 ± 2.60 nM to 11.32 ± 1.59 nM, respectively, and Vildagliptin (4.79±1.66 IC50 nM) was used as a standard. The most active derivative substituted Oxadiazole of pyrrolidine sulfonamide is B-XI (11.32 ± 1.59 IC50 nM) among all synthesized compounds. Conclusion: B-XI derivative has shown appreciable DPP-IVinhibitory action. The 1,2,4-oxadiazol-3-yl pyrrolidine-1-sulfonamide derivatives have shown anti-diabetic properties.

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Synthesis, Characterization, and Evaluation of in vitro Antidiabetic Activity of Novel Pyrrolidine Sulphonamide Derivative
Published
2021-12-28
How to Cite
1.
Salve M, Jadhav S. Synthesis, Characterization, and Evaluation of in vitro Antidiabetic Activity of Novel Pyrrolidine Sulphonamide Derivative. ijpi [Internet]. 28Dec.2021 [cited 18Aug.2022];11(4):374-8. Available from: https://jpionline.org/index.php/ijpi/article/view/1124