Novel benzothiazole based sulfonylureas/sulfonylthioureas: design, synthesis and evaluation of their antidiabetic potential

作者：Kharbanda Chetna; Alam Mohammad Sarwar^*; Hamid Hinna^*; Javed Kalim; Bano Sameena; Ali Yakub; Dhulap Abhijeet; Alam Parwez; Pasha M A Q

来源：New Journal of Chemistry, 2016, 40(8): 6777-6786.

DOI：10.1039/c5nj03589a

In the present study, twenty-eight benzothiazole based sulfonylureas/sulfonylthioureas were synthesized and were assessed for their antidiabetic effect in a normoglycemic rat model by the in vivo oral glucose tolerance test (OGTT). All the synthesized compounds were studied for their interactions inside the PPAR-gamma receptor site through a docking study. Subsequently, in vitro PPAR-gamma transactivation assay was performed on ten active compounds 7c, 7d, 7i-l, 8c, 8d, 8g, and 8h which showed potent antidiabetic activity in the OGTT (better than standard drugs) and also showed a good dock score with the PPAR-gamma receptor site. These active ten compounds were also found to transactivate PPAR and therefore were assessed for their antidiabetic potential on the STZ induced diabetic model. Effects of these compounds on body weight were also monitored during the course of study. Furthermore, the most effective compound 7j was evaluated for its effect on PPAR-gamma gene expression.

• 出版日期2016-8