Potent, selective human β 3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore

…, MR Candelore, MA Cascieri, L Deng, L Tota…

文献索引：Mathvink; Barritta; Candelore; Cascieri; Deng; Tota; Strader; Wyvratt; Fisher; Weber Bioorganic and medicinal chemistry letters, 1999 , vol. 9, # 13 p. 1869 - 1874

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被引用次数: 60

摘要

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.