Aim/Background: There is an increasing prevalence of diabetes mellitus throughout the world, and new compounds are necessary to combat this. While the current available antidiabetic therapies are long-term complicated and side effects-prone, this has led to a demand for more affordable, more effective methods of tackling diabetes. Research is focused on finding alternative medicinal remedies with significant antidiabetic efficacy as well as low adverse effects. This study synthesized, characterized, and evaluated anti-diabetic properties of synthetic sulphonamide hybrid of 1,3,4-oxadiazole derivatives. Materials and Methods: An in vivo antihyperglycemic evaluation of the sulphonamide hybrid of 1,3,4-oxadiazole derivatives was conducted using wistar rat models of type II diabetes derived from a two-step synthesis. Our study examined the effects of synthesized compounds on a model induced by a high-fat diet combined with streptozotocin and nicotinamide injection. For assessment of diabetic effects, Vildagliptin (10 mg/kg/day) was used as the standard drug. On day 14 th , 1,3,4-oxadiazole derivatives (50 mg/kg/day) significantly lowered the blood sugar of hyperglycemic rats. Results: Due HFD STZ with Nicotinamide blood glucose level of wistar rat was increased (295 ± 8.2). After 14 th day administration of derivatives random blood glucose level under controlled. A-III (220± 7.5 B) and A-IV (222 ± 3.62 B) were lowered random blood glucose levels on wistar rat. As compared to diabetes control (295 ± 8.5), derivatives of 1,3,4-oxadiazole are considered promising lead compounds. Compounds A-III and A-IV were found to be the most effective in lowering blood glucose, indicating the potential of these compounds as antidiabetic agents. Conclusion: Hybrids developed in this study provide new classes of anti-diabetic agents, and further optimization can be performed using this information.
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, 1 H NMR, C 13 NMR, mass spectroscopy, elemental analysis, and screened for in vitro assay of DPP-IV inhibition. Results and Discussion: The IC 50 was calculated for compounds B-I, B-V, B-VI, B-XI, and B-XIII that inhibited enzymes significantly, IC 50 values ranging from 19.65 ± 2.60 nM to 11.32 ± 1.59 nM, respectively, and Vildagliptin (4.79±1.66 IC 50 nM) was used as a standard. The most active derivative substituted Oxadiazole of pyrrolidine sulfonamide is B-XI (11.32 ± 1.59 IC 50 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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