Synthesis and structure-activity relationship studies of phenolic hydroxyl derivatives based on quinoxalinone as aldose reductase inhibitors with antioxidant activity

详细信息    查看全文

• 作者：Xin Hao ; Zhongfei Han ; Yang Li ; Chenying Li ; Xing Wang ; Xin Zhang ; Qin Yang ; Bing Ma ; Changjin Zhu ; ^{zcj@bit.edu.cn}
• 关键词：Aldose reductase inhibitors ; Antioxidant activity ; Quinoxalinones ; Phenolic hydroxyl
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：27
• 期：4
• 页码：887-892
• 全文大小：1208 K
• 卷排序：27

文摘

Novel aldose reductase inhibitors exhibiting antioxidant activity were designed and synthesized based on quinoxalin-2(1H)-one scaffold. Phenolic hydroxyl containing compounds 6b and 6f exhibited not only significant ALR2 inhibition and selectivity but also antioxidant properties. Structure-activity relationship and docking studies further confirmed the importance of phenolic hydroxyl for enhancing ALR2 inhibitory activity and adding an antioxidant property.