Discovery of potent and orally bioavailable N, N′-diarylurea antagonists for the CXCR2 chemokine receptor

…, JD Elliott, RM Goodman, M Burman, HM Sarau…

Index: Jin, Qi; Nie, Hong; McCleland, Brent W.; Widdowson, Katherine L.; Palovich, Michael R.; Elliott, John D.; Goodman, Richard M.; Burman, Miriam; Sarau, Henry M.; Ward, Keith W.; Nord, Melanie; Orr, Bonnie M.; Gorycki, Peter D.; Busch-Petersen, Jakob Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 17 p. 4375 - 4378

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Citation Number: 34

Abstract

A series of 3-substituted N, N′-diarylureas was prepared and the structure–activity relationship relative to CXCR2 receptor affinity as well as their pharmacokinetic properties were examined. In vitro microsomal metabolism studies indicated that the lower clearance rates of the 3-sulfonamido-substituted compounds were most likely due to the suppression of glucuronidation.