ABSTRACT

GANGADHARA ANGAJALA and RADHAKRISHNAN SUBASHINI

Abstract ................................................................................................. 231 5.1 Introduction .................................................................................. 231 5.2 Experimental Work ...................................................................... 235 5.3 Antihyperglycemic Activity Evaluation ....................................... 238

5.3.1 Selection of Animal and Induction of Diabetes ............... 238 5.3.2 Chemicals ......................................................................... 238 5.3.3 Induction of Diabetes Mellitus ........................................ 239 5.3.4 Experimental Design ........................................................ 239 5.3.5 Histopathological Study ................................................... 240 5.3.6 Statistical Analysis ........................................................... 240 5.3.7 Hypoglycemic Effect of Synthesized Compounds .......... 240

5.4 Docking Studies ........................................................................... 241 5.5 Discussion and Results ................................................................ 243 5.6 Conclusion ................................................................................... 244

Keywords .............................................................................................. 244 Acknowledgment .................................................................................. 244 References ............................................................................................. 245

ABSTRACT

The diabetes mellitus represents one of the most common endocrine disorders usually affecting nearly 6% people of the total world’s population. India, the world’s second most populous country now has more people with type-2 diabetes than any other nation. Thiazolidinedione’s (TZDs) are an important classof antidiabetic drugs used for the treatment of type-2 diabetes mellitus. Novel 2,4-thiazolidinedione derivatives plays an important role in the design and discovery of active pharmacological agents. The compounds containing TZD nucleus shows promising activity in various categories such as antihyperglycemic, aldose reductase inhibitors, anti-arthritics, antiinflammatory, and anticancer and so on. In this fast moving generation, more and more new drugs containing TZD nucleus have been reported by various scientist sall over the world. Biological importance of TZDs as an effective antihyperglycemic agents are available in literature in the form of short reviews, so there is a need to couple the latest information available in literature on the synthesis of novel 2,4-thiazolidinedione derivatives in order to better understand the current status of this nucleus for medicinal research and development.The synthesis of various novel 2,4-thiazolidinedione derivatives containing sulfonylurea’s, flavonyl, and phthalazinone moieties are described along with their antihyperglycemic studies. The docking studies of the novel TZD were also performed in the active site of peroxisome proliferator-activated receptor gamma (PPARγ) receptor by using Molegro virtual docker.