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新型联苯磺酰胺衍生物作为选择性AT受体拮抗剂的设计、合成及生物学评价

Design, synthesis and biological evaluation of novel biphenylsulfonamide derivatives as selective AT receptor antagonists.

作者信息

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

机构信息

College of Pharmacy, Anhui University of Chinese Medicine, Hefei, China.

Anhui Province Key Laboratory of Chinese Medicinal Formula, Hefei, Anhui, China.

出版信息

Front Chem. 2022 Aug 26;10:984717. doi: 10.3389/fchem.2022.984717. eCollection 2022.

Abstract

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

摘要

已经设计并合成了一系列新型的选择性作用于AT受体的苯磺酰胺衍生物。分别通过放射性配体结合分析和细胞神经突生长试验评估结合亲和力和功能活性。化合物、、、、、和对AT受体表现出适度的选择性和亲和力。其中,表现出激动剂活性,并且与对AT受体表现出相似的选择性。进行分子对接以分析化合物与AT受体之间的结合模式和结合位点,为进一步开发提供参考。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4e9/9458978/997860e8d561/fchem-10-984717-g001.jpg

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