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

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URI
http://hdl.handle.net/11287/619056
Author
Allen, D. R.
Bolt, Amanda H.
Chapman, G. A.
Knight, R. L.
Meissner, J. W. G.
Owen, D. A.
Watson, R. J.
Date
2007-02-01
Journal
Bioorganic & medicinal chemistry letters
Type
Journal Article
Publisher
Elsevier
DOI
10.1016/j.bmcl.2006.10.088
Rights
Archived with thanks to Bioorganic & medicinal chemistry letters
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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.
Citation
Identification and structure-activity relationships of 1-aryl-3-piperidin-4-yl-urea derivatives as CXCR3 receptor antagonists. 2007, 17 (3):697-701 Bioorg. Med. Chem. Lett.
Publisher URL
http://www.sciencedirect.com/science/article/pii/S0960894X06012832
Note
This article is freely available via Open Access. Click on the 'Additional Link' above to access the full-text from the publisher's site.
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