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Peer-Reviewed Publication
Bioorg Chem2021;110104755.May 1, 2021Journal Article

Design and synthesis of novel glycyrrhetin ureas as anti-inflammatory agents for the treatment of acute kidney injury.

Hongbo Wang1, Jiawei Zuo2, Liang Zha3, Xia Jiang3, Caixia Wu1, Yong-An Yang4, Wenjian Tang5, Tianlu Shi6
1Department of Pharmacy, Shandong Medical College, Linyi 276000, China.
2First Affiliated Hospital of USTC, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, Anhui, 230001, China; School of Pharmacy, Anhui Medical University, Hefei 230032, China.
3School of Pharmacy, Anhui Medical University, Hefei 230032, China.
4Elion Nature Biological Technology Co., Ltd, Nanjing 210038, China.
5Department of Pharmacy, Shandong Medical College, Linyi 276000, China; School of Pharmacy, Anhui Medical University, Hefei 230032, China. Electronic address: ahmupharm@126.com.
6First Affiliated Hospital of USTC, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, Anhui, 230001, China. Electronic address: tianlu828@163.com.

Abstract

To develop new anti-inflammatory drugs for the prevention and treatment of acute kidney injury, a series of novel glycyrrhetic ureas were designed, synthesized and evaluated for anti-inflammatory activity using RAW264.7 cells. Compounds 5r-5u (2.04, 2.50, 3.25 and 2.48 μM, respectively) with acidic or neutral amino acid showed potent anti-inflammatory activity (IC50 = 2-3 μM for NO inhibition), am…

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