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

Bioorganic & Medicinal Chemistry Letters
Qi JinJakob Busch-Petersen

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.

References

Nov 27, 1999·Drug Metabolism Reviews·A Radominska-PandyaP I Mackenzie

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Citations

Aug 31, 2012·Journal of Medicinal Chemistry·James Pease, Richard Horuk
Feb 18, 2006·The Journal of Clinical Investigation·Jörg ReutershanKlaus Ley
Aug 16, 2015·Current Diabetes Reports·Antonio CitroLorenzo Piemonti
Jul 15, 2015·Journal of Chemical Information and Modeling·Helen HaNouri Neamati
Dec 3, 2014·Bioorganic & Medicinal Chemistry Letters·Hongfu LuFeng Ren
Oct 9, 2013·SAR and QSAR in Environmental Research·M Konstantinidou, D Hadjipavlou-Litina
Jan 24, 2007·Bioorganic & Medicinal Chemistry Letters·Brent W McClelandJakob Busch-Petersen
Aug 29, 2006·Bioorganic & Medicinal Chemistry Letters·Hong NieJakob Busch-Petersen
Nov 28, 2013·Pharmaceuticals·Laura M CampbellDavid J J Waugh
Jul 23, 2009·Chemistry : a European Journal·Frédéric BruyneelJacqueline Marchand-Brynaert
Nov 8, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Eugènia PujolSantiago Vázquez
Oct 27, 2009·Bioorganic & Medicinal Chemistry·Pancham BakshiMichael Mullan

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