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 ,
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
