Synthesis and biological evaluation of novel dimethyl[1,1¡ä-biphenyl]-2,2¡ä-dicarboxylate derivatives containing thiazolidine-2,4-dione for the treatment of concanavalin A-induced acute liver injury of BALB/c mice

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• 作者：Guangcheng Wang^a ; ^c ; ¹ ; Chongyang Deng^a ; ¹ ; Caifeng Xie^a ; Liang Ma^a ; Jincheng Yang^a ; ^c ; Neng Qiu^a ; Qinyuan Xu^a ; Tao Chen^a ; Fei Peng^a ; Jinying Chen^a ; Jingxiang Qiu^a ; Aihua Peng^a ; ^b ; ^{peng_aihua@163.com} ; Yuquan Wei^a ; Lijuan Chen^a ; ^b ; ^{lijuan17@hotmail.com}
• 关键词：Anti-inflammation ; Hepatoprotective ; Thiazolidine-2 ; 4-dione ; Bifendate
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：December, 2011
• 年：2011
• 卷：46
• 期：12
• 页码：5941-5948
• 全文大小：1697 K

文摘

In this paper, we reported the synthesis of bifendate derivatives and evaluation of anti-inflammatory activity by detecting the production of the Nitric Oxide (NO) in the lipopolysaccharide(LPS)-stimulated RAW 264.7 cell lines. Among the newly derivatives, compound 7k was the most potent one and two other compounds (7e and 7f) also exhibited greater anti-inflammatory activity than bifendate. Further in?vivo studies confirmed that 7k significantly and dose-dependently inhibited carrageenan-induced paw edema and decreased the serum levels of alanine aminotransaminase, and aspartate aminotransaminase in concanavalin A-induced hepatitis model. Histopathological evaluation demonstrated that 7k has better hepatoprotective effect on acute liver injury induced by concanavalin A than bifendate, suggesting that 7k is a potential drug candidate for the treatment of hepatic injuries.