544716-08-7Relevant articles and documents
CYCLOALKYL ACID DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL APPLICATION THEREOF
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, (2016/11/14)
The present invention relates to a cycloalkyl acid derivative, a preparation method thereof, and a pharmaceutical application thereof, and in particular, the present invention relates to a cycloalkyl acid derivative represented by general formula (I) and a medical salt thereof, a preparation method thereof, and an application of the cycloalkyl acid derivative and the medical salt thereof as URAT1 inhibitors, and particularly as therapeutic agents for diseases related to an abnormal uric acid level, wherein definitions of substituent groups in general formula (I) are the same as definitions in the specifications.
Discovery of potent and orally bioavailable inhibitors of Human Uric Acid Transporter 1 (hURAT1) and binding mode prediction using homology model
Peng, Jianbiao,Hu, Qiyue,Gu, Chunyan,Liu, Bonian,Jin, Fangfang,Yuan, Jijun,Feng, Jun,Zhang, Lei,Lan, Jiong,Dong, Qing,Cao, Guoqing
supporting information, p. 277 - 282 (2016/01/09)
This Letter describes the discovery of a series of potent inhibitors of Human Uric Acid Transporter 1 (hURAT1). Lead generation and optimization via 3D pharmacophore analysis resulted in compound 41. With an IC50 of 33.7 nM, 41 also demonstrated good oral bioavailability in rat (74.8%) and displayed a consistent PK profile across all species tested (rat, dog and monkey).