Design, Synthesis and In-vivo Hypoglycemic Evaluation of Novel Non - TZD’S in a Type - 2 Diabetic Model

Title:Design, Synthesis and In-vivo Hypoglycemic Evaluation of Novel Non - TZD’S in a Type - 2 Diabetic Model

Volume: 9 Issue: 1

Author(s): Rupali Jadhav, Ranu Gupta-Rajoria, Tanushree Pal and Ramaa Chelakara Subramanian

Affiliation:

Keywords: 4-benzylidene-3, 5-isoxazolidinedione, docking, HFD- low STZ model, hypoglycemic activity , Knoevenagel condensation

Abstract: With a view to develop novel non-TZD anti-diabetic compounds, series of isoxazolidinediones were designed to target the PPAR-γ receptors. Docking studies were performed on co-crystallized protein structure of rosiglitazone with PPAR-γ receptor obtained from Protein Data Bank (2PRG). Interactions similar to that of rosiglitazone were observed for three molecules; 3a, 3b and 3c which were further synthesized and subjected to in vivo hypoglycemic, total cholesterol (CHL) and triglyceride (TG) evaluation. 14 days treatment revealed significant reduction in blood glucose levels but did not portray desirable results in terms of total CHL and TG lowering effect. The blood glucose reduction observed for 3a, 3b and 3c at 20 mg/kg/day was 53.96 %, 61.35%, 61.32% respectively as against 59.95% of the standard pioglitazone at 10mg/kg/day.

Cite this article as:

Jadhav Rupali, Gupta-Rajoria Ranu, Pal Tanushree and Chelakara Subramanian Ramaa, Design, Synthesis and In-vivo Hypoglycemic Evaluation of Novel Non - TZD’S in a Type - 2 Diabetic Model, Medicinal Chemistry 2013; 9 (1) . https://dx.doi.org/10.2174/1573406411309010104