Systematic structure-activity relationship(SAR) exploration of a moderately active tetrazole-bearmg lesinurad-based hit If led to the discovery of a potent uric acid transporter I(URAT1) inhibitor li, which posses...Systematic structure-activity relationship(SAR) exploration of a moderately active tetrazole-bearmg lesinurad-based hit If led to the discovery of a potent uric acid transporter I(URAT1) inhibitor li, which possessed a novel molecular skeleton and was 11-fold more potent than the parent lesinurad against human URAT1 in-vitro (IC50=0.66 gmol/L for li vs. 7.18 μmol/L for lesinurad).展开更多
基金Supported by the Key Projects of Tianjin Science and Technology Support Plan, China(No. 16YFZC SY00910) and the Natu- ral Science Foundation of Shandong Province, China(No.ZR2015BM028).
文摘Systematic structure-activity relationship(SAR) exploration of a moderately active tetrazole-bearmg lesinurad-based hit If led to the discovery of a potent uric acid transporter I(URAT1) inhibitor li, which possessed a novel molecular skeleton and was 11-fold more potent than the parent lesinurad against human URAT1 in-vitro (IC50=0.66 gmol/L for li vs. 7.18 μmol/L for lesinurad).