标题：A Systematic Review of Uric Acid Transporter 1 (URAT1) Inhibitors for the Treatment of Hyperuricemia and Gout and an Insight into the Structure-activity Relationship (SAR)
作者：Cai Wen-Qing; Liu Wei; Liu Chang-Ying; Wang Jian-Wu; Zhao Gui-Long
作者机构：[Wen-Qing, C] School of Chemistry and Chemical Engineering, Shandong University, Jinan, 250100, China, Tianjin Key Laboratory of Molecular Design and 更多
通讯作者地址：[Wang, JW]Shandong Univ, Sch Chem & Chem Engn, Jinan 250100, Peoples R China;[Zhao, GL]Tianjin Inst Pharmaceut Res, Tianjin Key Lab Mol Design & Drug 更多
关键词：gout;hyperuricemia;urate-lowering therapy;uricosuric;URAT1 inhibitor;structure-activity relationship (SAR)
摘要：Gout is caused by the deposition of uric acid as monosodium urate (MSU).Chronic hyperuricemia is the necessary condition for MSU deposition,which arises from over-production and/or under-excretion of uric acid.Renal under-excretion of uric acid accounts for greater than 90％ of the patients with hyperuricemia,making URATI inhibitors,which act through uricosuric effect a promising class of urate-lowering therapy (ULT).This review aims at the summary and discussion of the latest development of URAT1 inhibitors for the treatment of hyperuricemia and gout and providing an insight into their structure-activity relationship (SAR),which will be helpful to the design of URAT1 inhibitors for both academic research and pharmaceutical industry.The current development pipeline of URAT1 inhibitors is promising and encouraging.