Research progress and medicinal chemistry strategies of URAT1 inhibitors
10.16438/j.0513-4870.2022-0573
- VernacularTitle:URAT1抑制剂研究进展及药物化学策略
- Author:
Xiao-yu SHI
;
Tong ZHAO
;
Jian ZHANG
;
Rui-peng LIANG
;
Zhi-jiao ZHANG
;
Xin-yong LIU
;
Peng ZHAN
- Publication Type:Research Article
- Keywords:
uric acid;
hyperuricemia;
gout;
lesinurad;
URAT1 inhibitor
- From:
Acta Pharmaceutica Sinica
2022;57(10):2960-2971
- CountryChina
- Language:Chinese
-
Abstract:
The urate transporter 1 (URAT1) which controls urate reabsorption is a membrane transporter in the apical membrane of human renal proximal tubule epithelial cells. It was found that about 90% of patients suffer from hyperuricemia due to insufficient uric acid excretion. Therefore, the development of URAT1 inhibitors that can reduce the level of serum uric acid in vivo by enhancing renal urate excretion has been a hot spot in seeking anti-gout drugs in recent years. In this article, the representative URAT1 inhibitors with uric acid-lowering or anti-gout effects are reviewed, and related medicinal chemical strategies are analyzed, hoping to provide valuable insights into the discovery of new URAT1 inhibitors.
