Human Uric Acid Transporter 1 (hURAT1): An Inhibitor Structure–Activity Relationship (SAR) Study
MF Wempe, B Quade, P Jutabha, T Iwen…
Index: Wempe; Quade; Jutabha; Iwen; Frick; Rice; Wakui; Endou Nucleosides, Nucleotides and Nucleic Acids, 2011 , vol. 30, # 12 p. 1312 - 1323
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Abstract
The current study describes the chemical synthesis of a series of (2-ethylbenzofuran-3- yl)(substituted-phenyl) methanone compounds and their subsequent in vitro testing via oocytes expressing hURAT1. The experimental data support the notion that a potent hURAT1 inhibitor requires an anion (ie, a formal negative charge) to interact with the positively charged hURAT1 binding pocket. An anion appears to be a primary requirement ...