Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 5, Pages 1573-1576Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.01.074
Keywords
chemokine; chemokine antagonist; CXCR3; IP-10; CXC-L10; multiple sclerosis; benzimidazole; 2-iminobenzimidazole; partial solubility
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High-throughput screening identified a low molecular weight antagonist of CXCR3 displaying micromolar activity in a membrane filtration-binding assay. Systematic modi. cation 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. (c) 2008 Elsevier Ltd. All rights reserved.
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