Benzisoxazole containing Thiazolidinediones as Peroxisome Proliferator Activated Receptor-γ Agonists: Design, Molecular Docking, Synthesis & anti-diabetic studies
Journal Title: Scholars Academic Journal of Pharmacy - Year 2014, Vol 3, Issue 1
Abstract
A series of novel benzisoxazole containing thiazolidinediones were designed, docked with PPAR-γ protein leading to identification of a highly potent PPAR-γ agonist, compound S7. Based on molecular docking studies and lipinski’s rule of five, nine analogues out of 12 were synthesized and characterized by FT-IR, 1H-NMR and Mass spectra. Anti-diabetic activity of nine analogues was evaluated in alloxan (70 mg/kg, i.v.)-induced diabetes in mice [single-dose one day study]. The molecular docking and the pharmacological studies revealed that the distances between the acidic group and the linker, when a ligand was complexed with PPAR-γ protein, are important for the potent activity. The acidic head part of S7 makes intensive hydrophobic interaction with the PPAR-γ protein resulting in potent activity. Keywords: Design, Molecular docking, PPAR-γ agonists, anti-diabetic activity.
Authors and Affiliations
Shriram S. Purohit, Veerapur V. P
Keywords
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