Presentation1_Design, synthesis and biological evaluation of novel biphenylsulfonamide derivatives as selective AT2 receptor antagonists.pdf

A novel series of benzenesulfonamide derivatives that selectively act on the AT₂ 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 AT₂ receptor. Among them, 8j exhibited agonist activity and 8l displayed similar selectivity to the AT₂ receptor with PD123,319. Molecular docking was carried out to analyze the binding mode and binding site between the compound and the AT₂ receptor to provide a reference for further development.