SYNTHESIS AND EVALUATION OF NOVEL THIAZOLIDINEDIONES FOR ANTI DIABETIC ACTIVITY

Research Article, Rekha, Shantharam
unpublished
The aim of our study was to review on synthesis and various pharmacological activities associated with thaizolidinediones. Thaizolidinediones serve as a boon in the antidiabetic therapy by increasing the sensitivity towards insulin. 1, 3-Thiazolidine-2, 4-dione contains basic skeleton of thiazole or thiazolidine. Presence of one carbonyl group in thiazole at 4 th position makes it thiazolidine-4-one which is known for various activities and presence of another carbonyl group at 2 nd position
more » ... at 2 nd position makes it thiazolidine-2, 4-dione which is basically known for its antidiabetic activity. The thiazolidinediones used in oral combination therapy in management of patients with type II diabetes are ligand-activated transcription factors belonging to the nuclear receptor super family. The two clinically used PPAR γ agonists pioglitozone and rosiglitazone have made a great contribution to the therapy of type II diabetes. However, weight gain and hepatotoxicity are side effects of thiazolidinedione. For lesser side effects, researchers are focusing on modification of side chain at C-5 position of thiazolidinedione nucleus and its derivatisation. The basic ring of thiazolidinedione was synthesized by 1, 3 dipolar cycloaddition of thiourea and monochloro acetic acid. Knoevenagel condensation with substituted aromatic aldehyde was carried out to yeild various substituted benzylidenethiazolidine-2, 4-dione. These compounds were subjected to further esterification and substitution reaction to yield our target compounds as described in scheme 1. The synthesised molecules were screened for blood glucose lowering effect (in vivo). Charcterisation was done by using various physicochemical and spectral techniques. IVa and IV b showed blood glucose lowering effect in dexamethasone induced insulin resistance model.
fatcat:ziohogpy3ndgjj4vc6eldmxlyi