Potent, elective human beta3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore. |
| |
| Authors: | R J Mathvink A M Barritta M R Candelore M A Cascieri L Deng L Tota C D Strader M J Wyvratt M H Fisher A E Weber |
| |
| Affiliation: | Department of Medicinal Chemistry and Biochemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. |
| |
| Abstract: | A series of compounds possessing an N-substituted indoline-5-sulfonamide pharmacophore was prepared and evaluated for their human beta3 adrenergic receptor agonist 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 beta1 binding and 1400-fold selectivity over beta2 binding. |
| |
| Keywords: | |
|
|
