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Synthesis and evaluation of sulfonamide derivatives as potent Human Uric Acid Transporter 1 (hURAT1) inhibitors.

Xintuo Yang, Xuehai Pang, Lei Fan, Xinghai Li, Yuanwei Chen

Bioorganic & medicinal chemistry letters 2017 May 01


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    This letter presents synthesis and structure-activity relationship study of sulfonamide derivatives as inhibitors of Human Uric Acid Transporter 1 (hURAT1). Among all tested sulfonamide derivatives, compounds 9b, 16i and 19b exhibited excellent inhibition activity with IC50 value of 10, 2, and 83nM, respectively. In addition, compounds 9b and 19b demonstrated moderate PK profile in rats. Copyright © 2017 Elsevier Ltd. All rights reserved.

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    Xintuo Yang, Xuehai Pang, Lei Fan, Xinghai Li, Yuanwei Chen. Synthesis and evaluation of sulfonamide derivatives as potent Human Uric Acid Transporter 1 (hURAT1) inhibitors. Bioorganic & medicinal chemistry letters. 2017 May 01;27(9):1919-1922

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    PMID: 28351592

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