Bioorganic and Medicinal Chemistry Letters p. 1101 - 1106 (1998)
Update date:2022-08-04
Topics: Molecular docking Cell Culture Chemical Synthesis Potent Selective Agonists Benzenesulfonamide Human β3 adrenergic receptor Biological assay
Weber, Ann E.
Mathvink, Robert J.
Perkins, Leroy
Hutchins, Jennifer E.
Candelore, Mari R.
Tota, Laurie
Strader, Catherine D.
Wyvratt, Matthew J.
Fisher, Michael H.
A cloned human β3 adrenergic receptor assay was used to identify phenoxypropanolamine agonist 1. SAR, studies led to the identification of benzenesulfonamide derivative 20, a 6.3 nM β3 agonist which shows 30-fold selectivity for β3 agonist activity over β1 and β2 receptor binding. Further refinement of this lead provided 4-bromo derivative 39, a subnanomolar agonist with 660-fold and 230-fold selectivity over β1 and β2, respectively.
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