摘要
黄嘌呤氧化酶抑制剂非布司他是经典的抗痛风药物,治疗效果显著且耐受性好。非布司他及其衍生物在结构上可以分为两个主要部分,分别为取代苯环和羧基取代的五元或六元杂环。本文综述了近10年来非布司他衍生物的研究进展,针对各类衍生物的构效关系进行了分类概述。探究黄嘌呤氧化酶抑制剂的作用机制和构效关系,对合理设计和开发抗痛风的新化学实体具有十分重要的意义。
Febuxostat,as a xanthine oxidase inhibitor,is a classic anti-gout drug with significant therapeutic effects and good tolerability.The structures of febuxostat and its derivatives can be divided into two parts:a substituted phenyl ring and a five-membered or six-membered heterocyclic ring with a carboxyl substitution.This paper reviewed the research progress of febuxostat derivatives in recent ten years and classified the structure-activity relationships of various febuxostat derivatives.Exploring the action mechanisms and structure-activity relationships of xanthine oxidase inhibitors might be significant for the rational design and development of new anti-gout chemical entities.
作者
李文烨
翟纳
巨修练
刘根炎
LI Wen-ye;ZHAI Na;JU Xiu-lian;LIU Gen-yan(Key Laboratory for Green Chemical Process of Ministry of Education,Hubei Key Laboratory of Novel Reactor and Green Chemical Technology,School of Chemical Engineering and Pharmacy,Wuhan Institute of Technology,Wuhan 430205,China)
出处
《药学学报》
CAS
CSCD
北大核心
2021年第12期3401-3413,共13页
Acta Pharmaceutica Sinica
基金
国家自然科学基金资助项目(22177090,21807082)
湖北省高等学校优秀中青年科技创新团队计划项目(T201908)
湖北省中央引导地方科技发展专项资金项目(2020ZYYD040)。
关键词
黄嘌呤氧化酶
抑制剂
非布司他
痛风
构效关系
xanthine oxidase
inhibitor
febuxostat
gout
structure-activity relationship
