A Systematic Review of Uric Acid Transporter 1(URAT1) Inhibitors for the Treatment of Hyperuricemia

• 作 者: 蔡文卿 刘巍 刘长鹰 王建武 赵桂龙
• 机 构: School of Chemistry and Chemical Engineering, Shandong University,Tianjin Key Laboratory of Molecula
• 出 处: 结构化学
• 发表日期: 2017年06期
• 关键词: urate excretion pharmaceutical lowering carboxylic pipeline helpful discussion p

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 URAT1 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.

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 URAT1 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.