Author/Authors :
Robert J. Mathvink، نويسنده , , Anna Maria Barritta، نويسنده , , Mari R. Candelore، نويسنده , , Margaret A. Cascieri، نويسنده , , Liping Deng، نويسنده , , Laurie Tota، نويسنده , , Catherine D. Strader، نويسنده , , Matthew J. Wyvratt Jr.، نويسنده , , Michael H. Fisher، نويسنده , , Ann E. Weber، نويسنده ,
Abstract :
A series of compounds possessing an N-substituted indoline-5-sulfonamide pharmacophore was prepared and evaluated for their human β3 adrenergic receptor agomost activity. The SAR of a wide range of urea and heterocyclic substituents is discussed. 4-Octyl thiazole compound 8c was the most potent and selective compound in the series, with 2800-fold selectivity over β1 binding and 1400-fold selectivity over β2 binding.
