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Bioorg Med Chem Lett. 2007 Feb 1;17(3):697-701. Epub 2006 Nov 2.

Identification and structure-activity relationships of 1-aryl-3-piperidin-4-yl-urea derivatives as CXCR3 receptor antagonists.

Author information

1
UCB, Inflammation Discovery, Granta Park, Great Abington, Cambridge CB21 6GS, UK.

Abstract

The synthesis and biological evaluation of a series of 1-aryl-3-piperidin-4-yl-urea derivatives as small-molecule CXCR3 antagonists is described. SAR studies resulted in significant improvement of potency and physicochemical properties and established the key pharmacophore of the series, and led to the identification of 9t, which exhibits an IC50 of 16 nM in the GTPgammaS35 functional assay.

PMID:
17097877
DOI:
10.1016/j.bmcl.2006.10.088
[Indexed for MEDLINE]

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