AUTHOR=Wang Danhui , Zhao Wenjie , Zhang Zuzhi , Zhang Yanchun , Li Jiaming , Huang Weijun 

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

JOURNAL=Frontiers in Chemistry

VOLUME=Volume 10 - 2022

YEAR=2022

URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2022.984717

DOI=10.3389/fchem.2022.984717

ISSN=2296-2646

ABSTRACT=A novel series of benzenesulfonamide derivatives that selectively act on AT2 receptor had been designed and synthesized. The binding affinity and functional activity were evaluated by radio-ligand binding analysis and cell neurite outgrowth assay with NG108-15 cells separately. The compounds 8d, 8h, 8i, 8j, 8l and 9h exhibited moderate selectivity and affinity for AT2 receptor. Among them, 8j exhibited agonist activity and 8l displayed similar selectivity to AT2 receptor with PD123,319. Molecular docking was carried out to analysis the binding mode and binding site between the compound and AT2 receptor to provide reference for further development.