Discovery of potent and orally bioavailable N, N′-diarylurea antagonists for the CXCR2 chemokine receptor
Q Jin, H Nie, BW McCleland, KL Widdowson… - Bioorganic & medicinal …, 2004 - Elsevier
Q Jin, H Nie, BW McCleland, KL Widdowson, MR Palovich, JD Elliott, RM Goodman…
Bioorganic & medicinal chemistry letters, 2004•ElsevierA 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.
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.
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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