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ID: ALA1137097

Journal: Bioorg Med Chem Lett

Title: Discovery of potent and orally bioavailable N,N'-diarylurea antagonists for the CXCR2 chemokine receptor.

Authors: Jin Q, Nie H, McCleland BW, Widdowson KL, Palovich MR, Elliott JD, Goodman RM, Burman M, Sarau HM, Ward KW, Nord M, Orr BM, Gorycki PD, Busch-Petersen J.

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.

CiteXplore: 15357956

DOI: 10.1016/j.bmcl.2004.06.097