Document Report Card
Basic Information
ID: ALA1130810
Journal: Bioorg Med Chem Lett
Title: Potent, selective benzenesulfonamide agonists of the human beta 3 adrenergic receptor.
Authors: Weber AE, Mathvink RJ, Perkins L, Hutchins JE, Candelore MR, Tota L, Strader CD, Wyvratt MJ, Fisher MH.
Abstract: A cloned human beta 3 adrenergic receptor assay was used to identify phenoxypropanolamine agonist 1. SAR studies led to the identification of benzenesulfonamide derivative 20, a 6.3 nM beta 3 agonist which shows 30-fold selectivity for beta 3 agonist activity over beta 1 and beta 2 receptor binding. Further refinement of this lead provided 4-bromo derivative 39, a subnanomolar agonist with 660-fold and 230-fold selectivity over beta 1 and beta 2, respectively.
CiteXplore: 9871716