Title of article
Discovery of small molecule benzimidazole antagonists of the chemokine receptor CXCR3
Author/Authors
Martin E. Hayes، نويسنده , , Grier A. Wallace، نويسنده , , Pintipa Grongsaard، نويسنده , , Agnieszka Bischoff، نويسنده , , Dawn M. George، نويسنده , , Wenyan Miao، نويسنده , , Michael J. McPherson، نويسنده , , Robert H. Stoffel، نويسنده , , David W. Green، نويسنده , , Gregory P. Roth، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
4
From page
1573
To page
1576
Abstract
High-throughput screening identified a low molecular weight antagonist of CXCR3 displaying micromolar activity in a membrane filtration-binding assay. Systematic modification of the benzimidazole core and tethered acetophenone moiety established tractable SAR of analogs with improved physicochemical properties and sub-micromolar activity across both human and murine receptors.
Keywords
Benzimidazole , Partial solubility , Multiple sclerosis , Chemokine , Chemokine antagonist , CXCR3 , CXCL10 , IP-10 , 2-Iminobenzimidazole
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799209
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