Design, synthesis and biological evaluation of novel biphenylsulfonamide derivatives as selective AT2 receptor antagonists

A novel series of benzenesulfonamide derivatives that selectively act on the AT 2 receptor have been designed and synthesized. The binding affinity and functional activity were evaluated by radio-ligand binding analysis and cell neurite outgrowth assay, respectively. The compounds 8d , 8h , 8i , 8j , 8l , and 9h exhibited moderate selectivity and affinity for the AT 2 receptor. Among them, 8j exhibited agonist activity and 8l displayed similar selectivity to the AT 2 receptor with PD123,319 . Molecular docking was carried out to analyze the binding mode and binding site between the compound and the AT 2 receptor to provide a reference for further development.