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

Abstract 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 IC 50 value of 10, 2, and 83 nM, respectively. In addition, compounds 9b and 19b demonstrated moderate PK profile in rats.