Title of article
Identification and structure–activity relationships of 1-aryl-3-piperidin-4-yl-urea derivatives as CXCR3 receptor antagonists
Author/Authors
Daniel R. Allen، نويسنده , , Amanda Bolt، نويسنده , , Gayle A. Chapman، نويسنده , , Roland L. Knight، نويسنده , , Johannes W.G. Meissner، نويسنده , , David A. Owen، نويسنده , , Robert J. Watson، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
5
From page
697
To page
701
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 GTPγS35 functional assay.
Keywords
Chemokine , CXCR3 , SAR , Antagonist
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797722
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