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.

Background: Approximately 80% of deaths in diabetic patients are attributable to cardiovascular disease (CVD), which in turn is highly correlated with diabetic dyslipidemia. Statins are drug of choice for raised LDL-C in treating dyslipidemia. The present study compares the efficacy and safety of rosuvastatin against commonly used atorvastatin in patients of type 2 diabetes mellitus with dyslipidemia, so as to guide the present treatment strategies in the management of the same in Indian population.Methods: The study was a single blinded study conducted in a district level tertiary care hospital attached to a medical teaching institute. Patients fulfilling the inclusion criteria were randomized in two groups. Group I received atorvastatin (10mg) and group II received rosuvastatin (5mg) at bedtime orally daily. Serum TC, serum LDL-C, serum HDL-C and serum TG were assessed on week 0, week 6 and week 12.Results: At the end of 12 weeks, the percentage reduction of LDL-C levels in atorvastatin group was 33.58% whereas in rosuvastatin group, it was 43.12%. The percentage reduction in total cholesterol (TC) in atorvastatin group was 24.85% while in rosuvastatin group, it was 30.8%. Rise in HDL-C levels in atorvastatin group was 7.1% whereas in rosuvastatin group, it was 11.16%. All these differences were statistically significant. There was no significant difference in reduction of TG levels between the two groups.Conclusions: Rosuvastatin 5mg causes greater reduction in LDL-C and TC, comparable reduction of TG and greater rise in HDL-C when compared with atorvastatin 10mg therapy.