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- W2890102078 abstract "AIM: To develop novel, potent, selective and orally active inhibitors of Dipeptidyl Peptidase IVwith Anti-Diabetic activity.OBJECTIVES: Identification of common Pharmacophore features responsible for inhibiting DPP-IVusing Hiphop module of Catalyst® software 4.11 from Accelrys. Devlopment and validation of quantitative Pharmacophore hypothesis for series ofDPP-IV receptor using Hypogen/Hyporefine module of Catalyst® software 4.11 fromAccelrys. Generation of 10,000 scaffolds from the drug using scaffold hopping technique. Prediction of activity for designed molecules using the Hyporefine model and toidentify novel and potent DPP IV receptor using Lipinski rule of five. The potent receptor inhibitors attained as results may be used as lead for drugdevelopment. From the lead molecule, the derivatives of the compounds which has higher score valuewere synthesised. Characterization of the synthesized compounds by UV, Infrared spectroscopy, NuclearMagnetic 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 ofsynthetic feasibility. Four compounds with top scores were synthesized, purified, characterized usingUV, IR and NMR spectroscopy and Mass spectrometry.These four compounds were subjected to acute toxicity studies to fix the LD50. TheLD50 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 determineantidiabetic activity and were found to decrease the blood glucose levels, but theydid not fare better than the standard drug glibenclamide." @default.
- W2890102078 created "2018-09-27" @default.
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- W2890102078 date "2012-05-01" @default.
- W2890102078 modified "2023-09-27" @default.
- W2890102078 title "Design, Synthesis, Characterization and Pharmacological Evaluation of DPP-IV Inhibitors for Antidiabetic Activity." @default.
- W2890102078 hasPublicationYear "2012" @default.
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