A new series of 5-[4-(substituted) benzylidene or benzyl] thiazolidine-2, 4-dione (TZDs) have been synthesized using economical synthetic routes. The aim of the synthesis based on modification of linker region and effector region of rosiglitazone. Among these newly synthesized compounds, based on their docking results, some compounds were selected for study of oral hypoglycemic activity on fructose induced hyperglycemia in Wistar rats. The results of selected compounds shows that, 5-[4-(2-amino-5-ethoxypyridine) sulphonyl benzylidene] thiazolidine-2, 4-dione and 5-[4-(2-amino-5-ethoxypyridine) ethoxy benzyl] thiazolidine-2, 4-dione have appreciable blood glucose-lowering effect compared to that of the reference drug, pioglitazone. Out of these two compounds, 5-[4-(2-amino-5-ethoxypyridine)ethoxy benzyl] thiazolidine-2, 4-dione shows better hydrogen bond interaction with amino acid residues of peroxisome proliferator activated receptor-gamma (PPARγ) and also shows better oral hypoglycemic activity in this series

Diabetes mellitus is a serious global health problem and taking its place as one of the main threats to human health in the 21 st century. The National Diabetes Information Clearinghouse & World Health Organization shows above 90% of the diabetic population fall under type 2 diabetes mellitus category. The treatment generally prescribed for type 2 diabetes mellitus has been a combination of diet, exercise and current therapeutic agents Due to their adverse effects and side effects, most of these treatments are considered to be unsatisfactory in terms of preventio n of complications and preservation of quality of life. The current therapeutic agents containing thiazolidine-2,4-diones or glitazones are shown better treatment on type 2 diabetes mellitus via acting on peroxisome proliferator-activated receptor-gamma (PPAR-γ). From these glitazones, troglitazone and rosiglitazone are withdrawn from markets. Pioglitazone and lobeglitazone are used in market. Ciglitazone, englitazone, darglitazone, KRP-297, rivoglitazone and CLX-921 are discontinued in various clinical trials. Mitoglitazone, netoglitazone and balaglitazone are present in various phases of clinical trials. Furthermore, based on various literature surveys, we are studied in details structure activity relationships of various glitazones.

Type 2 diabetes mellitus and its complications, decreases the quality of life in diabetic patients. Thiazolidine-2,4-diones are found to be better insulin sensitizing agents, acting on peroxisome proliferator activated receptor-γ (PPAR-γ) and decrease blood glucose level in diabetic patient. Therefore, in the present work, we synthesized 5-[4-(substituted) sulphonylbenzylidene]thiazolidine-2,4-diones and evaluated for their oral hypoglycemic activity. The synthesized compounds were further studied for their find out interactions with 2PRG protein with the help of docking score and also find out their predicated ED25 values. The results of synthesized compounds were showed significant decrease in blood glucose level as compared to positive control group. All synthesized compounds have shown good hydrogen bond interactions with 2PRG protein, docking score and predicted ED25 value as compared with reference drug, pioglitazone and rosiglitazone, respectively. Thus, sulphonyl linked thiazolidine-2,4-diones may be used as promising oral hypoglycemic agent.

A series of 1, 3-thiazolidin-4-one analogues were synthesized using microwave and structurally characterized by various spectroscopic techniques and elemental analysis. All synthesized compounds were screened for anticancer activity by sulforhodamine B (SRB) assay while in vitro anti-inflammatory activity was by inhibition of albumin denaturation technique. The compounds 5j, 5k, 5l, 5m, 5n were found to show significant anticancer and in vitro anti-inflammatory activity. Furthermore, molecular modelling studies of all molecules (5a-5s) were performed using V Life MDS software. Based on this it is observed that, compound 5m shows more stable complex with Polo-like kinase 1 by forming hydrogen bond and hydrophobic interactions. Finally it is concluded that, 1, 3-thiazolidin-4-one analogues shows anticancer and anti-inflammatory activity possibly because of inhibition of Pololike kinase 1.