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  • Title: Discovery of potent and orally bioavailable N,N'-diarylurea antagonists for the CXCR2 chemokine receptor.
    Author: 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.
    Journal: Bioorg Med Chem Lett; 2004 Sep 06; 14(17):4375-8. PubMed ID: 15357956.
    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.
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