Discovery of small molecule benzimidazole antagonists of the chemokine receptor CXCR3

…, P Grongsaard, A Bischoff, DM George, W Miao…

Index: Hayes, Martin E.; Wallace, Grier A.; Grongsaard, Pintipa; Bischoff, Agnieszka; George, Dawn M.; Miao, Wenyan; McPherson, Michael J.; Stoffel, Robert H.; Green, David W.; Roth, Gregory P. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 5 p. 1573 - 1576

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Citation Number: 30

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.