New Oxadiazolidinedione Derivatives as Potent and Selective Human β3 Agonists.

Abstract As part of our investigation into the development of potent and selective human β 3 agonists, a series of thiazolidinedione analogues was prepared and evaluated for their biological activity on the human β 3 -adrenergic receptor. The oxadiazolidinedione derivative 17 was found to be the most potent and selective compound in this study, with an EC 50 value of 0.02 μM at the β 3 receptor, 259-fold selectivity over the β 1 receptor, and 745-fold selectivity over the β 2 receptor.