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Design, synthesis and biological evaluation of inhibitors of urate transporter 1 (URAT1)
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Yong-cheng WANG, Ya-jun YANG, Xian-xin HOU, Ying YANG, Zhi-yan XIAO*
Acta Pharmaceutica Sinica | 2019, 54(6) : 1069 - 1074
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Acta Pharmaceutica Sinica | 2019, 54(6): 1069-1074
• Original Articles •
Design, synthesis and biological evaluation of inhibitors of urate transporter 1 (URAT1)
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Yong-cheng WANG, Ya-jun YANG, Xian-xin HOU, Ying YANG, Zhi-yan XIAO*
Affiliations
  • Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2019-06-12 doi: 10.16438/j.0513-4870.2019-0208
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Urate transporter 1 (URAT1) is a validated target for the treatment of hyperuricemia. Based on the structure of URC-102, which is currently under a phase Ⅱ clinical trial, fourteen novel analogs were designed and synthesized. Among them, four compounds (9b, 9c, 10e and 10g) exhibited substantial inhibitory effect against URAT1. The most active compound 9b showed an IC50 value of 0.061 μmol·L-1, which is significantly more potent than Lesinurad and Benzbromarone. Preliminary SAR was drawn, providing clues for further structural optimization.

URAT1 inhibitors  /  hyperuricemia  /  gout  /  URC-102 analogs
Yong-cheng WANG, Ya-jun YANG, Xian-xin HOU, Ying YANG, Zhi-yan XIAO. Design, synthesis and biological evaluation of inhibitors of urate transporter 1 (URAT1)[J]. Acta Pharmaceutica Sinica, 2019 , 54 (6) : 1069 -1074 . DOI: 10.16438/j.0513-4870.2019-0208
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Article Info
doi: 10.16438/j.0513-4870.2019-0208
  • Receive Date：2019-03-27
  • Online Date：2026-01-26
  • Published：2019-06-12
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  • Received：2019-03-27
  • Revised：2019-04-15
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    Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
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小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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