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

A series of compounds possessing an N-substituted indoline-5-sulfonamide pharmacophore was prepared and evaluated for their human β 3 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...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1999-07, Vol.9 (13), p.1869-1874
Main Authors: Mathvink, Robert J, Barritta, Anna Maria, Candelore, Mari R, Cascieri, Margaret A, Liping Deng, Tota, Laurie, Strader, Catherine D, Wyvratt, Matthew J, Fisher, Michael H, Weber, Ann E
Format: Article
Language:English
Subjects:
Biological and medical sciences
Catecholaminergic system
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
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Summary:A series of compounds possessing an N-substituted indoline-5-sulfonamide pharmacophore was prepared and evaluated for their human β 3 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 β 1 binding and 1400-fold selectivity over β 2 binding. Graphic
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(99)00277-2