Thiazaheterocycles such as thiazole and thiazolidine-2,4-dione, are privileged structures which shows several pharmacological activities. In this research, we used these scaffolds in order to get new antidiabetic compounds. A series of thiazolidine-2,4-dione (TZD) and related bioisosteres were prepared and their in vitro relative expression of PPAR alpha,  PPAR gamma were determinate. Some compounds showed an increase in the mRNA expression of both PPAR isoforms, as well as the GLUT-4 levels and FATP-1. Thiazole derivatives were tested as 11�-HSD1 inhibitors. The antidiabetic activity of the most active compounds of each series was determined at 50 mg/Kg single oral dose using a non-insulin dependent diabetes mellitus rat model. The results indicated a significant decrease in plasma glucose levels.

Thiazaheterocycles with antidiabetic activity: Design, synthesis, and in combo pharmacological studies

248th National Meeting (2014)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.