Author/Authors :
Baihua Hu، نويسنده , , Michael Malamas، نويسنده , , John Ellingboe، نويسنده , , Elwood Largis، نويسنده , , Stella Han، نويسنده , , Ruth Mulvey، نويسنده , , Jeff Tillett، نويسنده ,
Abstract :
As part of our investigation into the development of potent and selective human β3 agonists, a series of thiazolidinedione analogues was prepared and evaluated for their biological activity on the human β3-adrenergic receptor. The oxadiazolidinedione derivative 17 was found to be the most potent and selective compound in this study, with an EC50 value of 0.02 μM at the β3 receptor, 259-fold selectivity over the β1 receptor, and 745-fold selectivity over the β2 receptor.
