新型黄嘌呤氧化酶抑制剂对痛风治疗的研究进展  

Research progress in novel xanthine oxidase inhibitors and treatment of gout

作　　者：靳生菊 周苗 张佳宁 葛宫慧 张廷剑[1] 孟繁浩[1] JIN Shengju;ZHOU Miao;ZHANG Jianing;GE Gonghui;ZHANG Tingjian;MENG Fanhao(School of Pharmacy,China Medical University,Shenyang Liaoning 110122,China)

机构地区：[1]中国医科大学药学院,辽宁沈阳110122

出　　处：《中国药物警戒》2024年第2期223-228,共6页Chinese Journal of Pharmacovigilance

基　　金：国家自然科学基金项目(82273785);大学生创新创业项目(X202310159024、S202210159006)。

摘　　要：目的研究黄嘌呤氧化酶(xanthine oxidase,XO)抑制剂与痛风治疗的进展。方法从母核结构、分子对接、药物活性、药代动力学等方面对小分子XO抑制剂以及痛风作用机制进行论述。结果在多种XO抑制剂结构类型中,羧酸类和酰胺类对XO的抑制效果显著,活性与托吡司他相当,可以作为今后XO抑制剂设计的重点。结论以期对羧酸类和酰胺类进行进一步的结构优化,发现更优异的XO抑制剂用于痛风治疗。Objective To summarize the recent progress in research on xanthine oxidase(XO)inhibitors.Methods Small molecule XO inhibitors were elaborated in terms of structural scaffold,molecular docking,activity and pharmacokinetics.Results Carboxylic acid and amide based XO inhibitors showed a favorable potential with activities comparable to those of topiroxostat,which could be a hotspot for future design of XO inhibitors.Conclusion It is expected that further structural optimization of carboxylic acids and amides will lead to the discovery of more effective XO inhibitors.

关 键 词：黄嘌呤氧化酶 抑制剂 痛风 高尿酸血症 嘌呤 降尿酸药物 

分 类 号：R977[医药卫生—药品]