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. 2007 Feb 1;17(3):697-701.
doi: 10.1016/j.bmcl.2006.10.088. Epub 2006 Nov 2.

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

Daniel R Allen  1 , Amanda Bolt, Gayle A Chapman, Roland L Knight, Johannes W G Meissner, David A Owen, Robert J Watson
Affiliations

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

Daniel R Allen et al. Bioorg Med Chem Lett. .

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.

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