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Potent, elective human beta3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide
R J Mathvink1, A M Barritta, M R Candelore
1Department of Medicinal Chemistry and Biochemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
Bioorganic & Medicinal Chemistry Letters
|July 16, 1999
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.