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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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
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author Wang, Danhui
Zhao, Wenjie
Zhang, Zuzhi
Zhang, Yanchun
Li, Jiaming
Huang, Weijun
author_facet Wang, Danhui
Zhao, Wenjie
Zhang, Zuzhi
Zhang, Yanchun
Li, Jiaming
Huang, Weijun
author_sort Wang, Danhui
collection PubMed
description 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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spelling pubmed-94589782022-09-10 Design, synthesis and biological evaluation of novel biphenylsulfonamide derivatives as selective AT(2) receptor antagonists Wang, Danhui Zhao, Wenjie Zhang, Zuzhi Zhang, Yanchun Li, Jiaming Huang, Weijun Front Chem Chemistry 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. Frontiers Media S.A. 2022-08-26 /pmc/articles/PMC9458978/ /pubmed/36092654 http://dx.doi.org/10.3389/fchem.2022.984717 Text en Copyright © 2022 Wang, Zhao, Zhang, Zhang, Li and Huang. https://creativecommons.org/licenses/by/4.0/This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
spellingShingle Chemistry
Wang, Danhui
Zhao, Wenjie
Zhang, Zuzhi
Zhang, Yanchun
Li, Jiaming
Huang, Weijun
Design, synthesis and biological evaluation of novel biphenylsulfonamide derivatives as selective AT(2) receptor antagonists
title Design, synthesis and biological evaluation of novel biphenylsulfonamide derivatives as selective AT(2) receptor antagonists
title_full Design, synthesis and biological evaluation of novel biphenylsulfonamide derivatives as selective AT(2) receptor antagonists
title_fullStr Design, synthesis and biological evaluation of novel biphenylsulfonamide derivatives as selective AT(2) receptor antagonists
title_full_unstemmed Design, synthesis and biological evaluation of novel biphenylsulfonamide derivatives as selective AT(2) receptor antagonists
title_short Design, synthesis and biological evaluation of novel biphenylsulfonamide derivatives as selective AT(2) receptor antagonists
title_sort design, synthesis and biological evaluation of novel biphenylsulfonamide derivatives as selective at(2) receptor antagonists
topic Chemistry
url 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
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