1. Academic Validation
  2. Comparison of N,N'-diarylsquaramides and N,N'-diarylureas as antagonists of the CXCR2 chemokine receptor

Comparison of N,N'-diarylsquaramides and N,N'-diarylureas as antagonists of the CXCR2 chemokine receptor

  • Bioorg Med Chem Lett. 2007 Mar 15;17(6):1713-7. doi: 10.1016/j.bmcl.2006.12.067.
Brent W McCleland 1 Roderick S Davis Michael R Palovich Katherine L Widdowson Michelle L Werner Miriam Burman James J Foley Dulcie B Schmidt Henry M Sarau Martin Rogers Kevin L Salyers Peter D Gorycki Theresa J Roethke Gary J Stelman Leonard M Azzarano Keith W Ward Jakob Busch-Petersen
Affiliations

Affiliation

  • 1 GlaxoSmithKline, 709 Swedeland Road, King of Prussia, PA 19406, USA.
Abstract

N,N'-diarylsquaramides were prepared and evaluated as antagonists of CXCR2. The compounds were found to be potent and selective antagonists of CXCR2. Significant differences in SAR was observed relative to the previously described N,N'-diarylurea series. As was the case in the N,N'-diarylurea series, placing sulfonamide substituent adjacent to the acidic phenol significantly reduced the clearance in rat pharmacokinetic studies.

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