异恶唑
化学
黄嘌呤氧化酶
化学合成
酶抑制剂
羧酸
立体化学
酶
组合化学
生物化学
体外
作者
Dongqian Huang,Wenye Li,Yilan Zhao,Cheng Xie,Xiaogang Luo,Fengshou Wu,Zhi‐Qiang Xu,Qi Sun,Genyan Liu
标识
DOI:10.1016/j.ejmech.2024.116443
摘要
Xanthine oxidase (XO) is a key enzyme for the production of uric acid in the human body. XO inhibitors (XOIs) are clinically used for the treatment of hyperuricemia and gout, as they can effectively inhibit the production of uric acid. Previous studies indicated that both indole and isoxazole derivatives have good inhibitory effects against XO. Here, we designed and synthesized a novel series of N-5-(1H-indol-5-yl)isoxazole-3-carboxylic acids according to bioisosteric replacement and hybridization strategies. Among the obtained target compounds, compound 6c showed the best inhibitory activity against XO with an IC
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