title: Design, synthesis and in-vivo hypoglycemic evaluation of novel non - TZD'S in a type - 2 diabetic model.
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.
authors: Bharati Vidyapeeth’s College of Pharmacy, Sector-8, C.B.D., Belapur, Navi Mumbai, Maharashtra, 400614, India.
authors: Rupali
authors: R
authors: Jadhav
authors: Ranu
authors: R
authors: Gupta-Rajoria
authors: Tanushree
authors: T
authors: Pal
authors: Ramaa Chelakara
authors: RC
authors: Subramanian
mesh_terms: D000818:Animals; D001786:Blood Glucose / Q000187:drug effects; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy*; D004195:Disease Models, Animal; D015195:Drug Design; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D008024:Ligands; D008958:Models, Molecular; D051381:Rats; D017207:Rats, Sprague-Dawley; D000077154:Rosiglitazone; D045162:Thiazolidinediones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D001786:Blood Glucose; D007004:Hypoglycemic Agents; D008024:Ligands; D045162:Thiazolidinediones; D000077154:Rosiglitazone