Synthesis and Evaluation of 1, 3-Thiazolidin-4-One Derivatives as Antihyperglycemic Agent (Research Article)

Author(s): Ranjithkumar Kadagandla and Baswaraju Macha

Abstract: Thiazolidinedione (TZD) class of drugs which were approved for the management of type 2 diabetes mellitus exemplified by rosiglitazone and pioglitazone (PG), act by modulation of PPARγ receptors. Rosiglitazone was found to induce heart failure due to fluid retention and hence it has been withdrawn from market. Concerns were also raised recently on the apparent risk of bladder cancer with the use of Pioglitazone. Based on the advances and better understanding of antidiabetic agents, rational approaches have been applied for further development of the newer antidiabetic agents. The dual agonists of PPAR-α/γ, PPAR-α/δ, PPAR-δα, PPAR pan agonists and selective PPARC modulators and partial agonists are cardinal attractive targets for medicinal chemists in this sojourn. Attempts were reported to develop such agents several modifications on thiazolidinedione ring and the substituents were made. This research paper presents the design of new series of thiazolidinones with pyridine/ pyrimidine tail and cyclopropylalkyl and aryl substituent with an ethoxy linker and their evaluation for antihyperglycemic activity. Some of the new thiazolidin-4-one derivatives were found to be equipotent to pioglitazone in lowering blood glucose in streptozotocin induced diabetic rats.

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