Design, synthesis and biological evaluation of novel biphenylsulfonamide derivatives as selective AT(2) 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, 8...

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Detalles Bibliográficos
Autores principales: Wang, Danhui, Zhao, Wenjie, Zhang, Zuzhi, Zhang, Yanchun, Li, Jiaming, Huang, Weijun
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2022
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9458978/
https://www.ncbi.nlm.nih.gov/pubmed/36092654
http://dx.doi.org/10.3389/fchem.2022.984717
Descripción
Sumario: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.

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