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    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
    Metadata
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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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