Srimathi, R (2012) Design, Synthesis, Characterization and Pharmacological Evaluation of DPP-IV Inhibitors for Antidiabetic Activity. Masters thesis, College of Pharmacy, Madras Medical College, Chennai.
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Abstract
AIM: To develop novel, potent, selective and orally active inhibitors of Dipeptidyl Peptidase IV with Anti-Diabetic activity. OBJECTIVES: Identification of common Pharmacophore features responsible for inhibiting DPP-IV using Hiphop module of Catalyst® software 4.11 from Accelrys. Devlopment and validation of quantitative Pharmacophore hypothesis for series of DPP-IV receptor using Hypogen/Hyporefine module of Catalyst® software 4.11 from Accelrys. Generation of 10,000 scaffolds from the drug using scaffold hopping technique. Prediction of activity for designed molecules using the Hyporefine model and to identify novel and potent DPP IV receptor using Lipinski rule of five. The potent receptor inhibitors attained as results may be used as lead for drug development. From the lead molecule, the derivatives of the compounds which has higher score value were synthesised. Characterization of the synthesized compounds by UV, Infrared spectroscopy, Nuclear Magnetic Resonance spectroscopy and Mass Spectroscopy. In vivo anti diabetic activity of synthesised compounds. CONCLUSION: Twenty five molecules which passed Lipinski’s rule were docked against DPP-4. The molecule containing purine and pyridine nucleus was selected on the basis of synthetic feasibility. Four compounds with top scores were synthesized, purified, characterized using UV, IR and NMR spectroscopy and Mass spectrometry. These four compounds were subjected to acute toxicity studies to fix the LD50. The LD50 value of the title compounds (SR A- SR D) was expected to exceed 50mg/kg. All the synthesised compound so were subjected to, invivo experiment to determine antidiabetic activity and were found to decrease the blood glucose levels, but they did not fare better than the standard drug glibenclamide.
| Item Type: | Thesis (Masters) |
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| Uncontrolled Keywords: | Design; Synthesis; Characterization; Pharmacological Evaluation; DPP-IV Inhibitors; Antidiabetic Activity |
| Subjects: | PHARMACY > Pharmaceutical Chemistry |
| Depositing User: | Ravindran C |
| Date Deposited: | 20 Oct 2017 06:45 |
| Last Modified: | 20 Oct 2017 06:45 |
| URI: | http://repository-tnmgrmu.ac.in/id/eprint/3707 |
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