Lead identification of 2-iminobenzimidazole antagonists of the chemokine receptor CXCR3

Bioorg Med Chem Lett. 2008 Apr 1;18(7):2414-9. doi: 10.1016/j.bmcl.2008.02.049. Epub 2008 Feb 26.

Abstract

Modification of a 2-iminobenzimidazole series derived from an HTS hit resulted in compounds with improved in-vitro species selectivity. Incorporation of an 8-quinoline amide and conformational rigidification of an aliphatic tether furnished potent compounds suitable for further lead optimization.

MeSH terms

  • Amides / chemistry
  • Amides / pharmacology*
  • Animals
  • Benzimidazoles / chemical synthesis
  • Benzimidazoles / pharmacology*
  • Binding Sites
  • CHO Cells / drug effects
  • Cricetinae
  • Cricetulus
  • Humans
  • Models, Chemical
  • Quinolines / chemistry
  • Quinolines / pharmacology*
  • Radioligand Assay
  • Receptors, CXCR3 / antagonists & inhibitors*
  • Receptors, CXCR3 / metabolism
  • Structure-Activity Relationship

Substances

  • Amides
  • Benzimidazoles
  • Quinolines
  • Receptors, CXCR3