Potent, selective benzenesulfonamide agonists of the human β3 adrenergic receptor

Article abstract of DOI:10.1016/S0960-894X(98)00169-3

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.