{"title":"Synthesis of Cyclopyrrolidine Clubbed with Oxadiazole Bases and Evaluation of their Anti-Diabetic Activity through in vivo Model","authors":"Salve Megha Tukaram, Jadhav Shailaja","doi":"10.5530/ijper.57.3s.85","DOIUrl":null,"url":null,"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.","PeriodicalId":13407,"journal":{"name":"Indian Journal of Pharmaceutical Education and Research","volume":" ","pages":""},"PeriodicalIF":0.8000,"publicationDate":"2023-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Indian Journal of Pharmaceutical Education and Research","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.5530/ijper.57.3s.85","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"EDUCATION, SCIENTIFIC DISCIPLINES","Score":null,"Total":0}
引用次数: 0
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.
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.