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Achaiah Garlapati

Achaiah Garlapati

Kakatiya University, India

Title: New thiazolidine-4-ones: Synthesis and evaluation for antidiabetic activity


Biography: Achaiah Garlapati


1,3-Thiazolidindiones (TZDs) are important class of antidiabetic agents which enhance insulin sensitivity of the target cells via activation of  Peroxisome Proliferator-Activated Receptor gamma (PPAR-γ), a nuclear receptor involved primarily in glucose homeostasis, adipogenesis, inflammatory diseases and certain types of cancers.1,3-Thiazolidindiones are associated with  various untoward effects, restricting their usage in the treatment of Type 2 diabetes. The main side effects of all TZDs are water retention, heart failure. Therefore, TZDs should be prescribed with both caution and patient warnings about the potential for water retention/weight gain, especially in patients with decreased ventricular function. The two TZDs, pioglitazone and rosiglitazone, are PPAR-γ agonists, do not cause serious liver damage, but do induce weight gain, fluid retention and heart failure and they have been associated with an increase in peripheral fractures in postmenopausal women, particularly in the humerus, hands and feet. Furthermore, it has been established that selective activation of PPAR-γ sub-type is primarily responsible for the observed undesirable effects. Therefore, partial agonists are considered a safer alternative to currently used thiazolidinediones (TZDs).
The attempt to develop such molecules, several modifications have been attempted in the tail and head groups of the TZDs to result in thiazolidin-4-ones and a few of them have been identified to possess potential antihyperglycemic activity.  The purpose of this study is to synthesize and screen new derivatives (General Structure) obtained by the incorporation of pyridine/pyrimidine in the tail and thiazolidine-4-one with cyclopropyl, alkyl, aryl groups etc. In place of R group and methyl and hydrogen in place of R1. Methodology: 4-[2-(Methyl-pyrimidin/pyridin-2-yl-amino)-ethoxy]-benzaldehyde (2) was prepared from 2-(methyl-pyrimidin/pyridin-2-yl-amino)-ethanol (1) and 4-fluorobenzaldehyde. The compound 2 in turn treated with appropriate amine and thioglycolic acid/ thiolactic acid to get the thiazolidine-4-ones. Findings: All the seven target molecules showed significant reduction in blood glucose levels in the streptozotocin induced diabetic rats at 4th and 6th Hrs after administration. Among the series, the compound with cyclopropyl group and pyridine moiety (IIg) showed comparable potency to that of the standard piogliazone at 6th hour (~55% reduction). Further, the activity increased with % reduction in blood glucose levels reaching 65.75 at 10th Hrs compared to 3% shown by standard indicating prolonged activity by the test compound.  Conclusion & Significance: The findings suggest that compound (IIg) could be further modified to improve the potency and tested for toxicity to identify safer molecules for further pre-clinical evaluation.