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Potent, selective human β3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore

1999; Elsevier BV; Volume: 9; Issue: 13 Linguagem: Inglês

10.1016/s0960-894x(99)00277-2

1464-3405

Robert J. Mathvink, Anna Maria Barritta, Mari R. Candelore, Margaret A. Cascieri, Liping Deng, Laurie Tota, Catherine D. Strader, Matthew J. Wyvratt, Michael H. Fisher, Ann E. Weber,

Pharmacological Effects and Assays

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.