Abstract
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.