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

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

文献索引：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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被引用次数: 34

摘要

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.