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

IF 0.8 4区 医学 Q3 EDUCATION, SCIENTIFIC DISCIPLINES Indian Journal of Pharmaceutical Education and Research Pub Date : 2023-08-23 DOI:10.5530/ijper.57.3s.85
Salve Megha Tukaram, Jadhav Shailaja
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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.
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恶二唑基环吡咯烷棒状化合物的合成及其体内抗糖尿病活性评价
背景和目的:基于DPP-IV抑制剂,有一种神奇的方法来开发抗糖尿病药物。这些抑制剂调节糖尿病患者的血糖水平,以防止他们的健康问题。在目前的工作中,我们创造了一系列新的化合物环吡咯烷与恶二唑碱的混合物。材料和方法:合成了恶二唑碱与环吡咯烷(B-1~B-16),并通过红外光谱、核磁共振、质谱和元素分析对其进行了表征。进行对接研究以评估受体DPP-4(PDB 3W2T)结合位点上合成命中物的相互作用和结合模式。以维达列汀为标准药物,对合成的六种化合物在HFD STZ烟酰胺诱导的糖尿病大鼠中的抗糖尿病活性进行了测试。结果:在HFD STZ烟酰胺中,化合物B-XIV(220*4.56B)与维达格利汀(215*7.52B)相比,在所有合成的化合物中导致血糖水平的最大降低。其他化合物显示出中等至良好的抗高血糖活性。结论:合成的化合物具有良好的DPP-IV抑制活性。含有吸电子基团(氯、硝基、甲氧基)的化合物比给电子基团(甲基、羟基)具有良好的抗糖尿病作用。恶二唑衍生物可用于进一步开发,以获得更有前景的候选药物。
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来源期刊
CiteScore
1.40
自引率
0.00%
发文量
227
审稿时长
>12 weeks
期刊介绍: The official journal of Association of Pharmaceutical Teachers of India (APTI) and is being published since 1967. IJPER, a quarterly publication devoted to publish reviews and research articles in pharmacy and the related disciplines of Pharmaceutical education. It mainly covers the articles of special interest, covering the areas of Pharmaceutical research, teaching and learning, laboratory innovations, education technology, curriculum design, examination reforms, training and other related issues. It encourages debates and discussions on the issues of vital importance to Pharmaceutical education and research. The goal of the journal is to provide the quality publications and publish most important research and review articles in the field of drug development and pharmaceutical education. It is circulated and referred by more than 6000 teachers, 40,000 students and over 1000 professionals working in Pharmaceutical industries, Regulatory departments, hospitals etc.
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