Discovery of new C3aR ligands. Part 1: arginine derivatives

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3258-61. doi: 10.1016/j.bmcl.2007.04.022. Epub 2007 Apr 10.

Abstract

The synthesis and in vitro binding of several new arginine-containing C3aR ligands are reported. DMPK properties and functional activities of selected compounds have been evaluated. One compound is shown to be active in an in vivo model of airway inflammation after aerosol administration.

MeSH terms

  • Aerosols / administration & dosage
  • Animals
  • Arginine / analogs & derivatives
  • Arginine / chemical synthesis
  • Arginine / pharmacology*
  • Complement Activation / drug effects*
  • Inflammation / chemically induced
  • Inflammation / pathology
  • Ligands
  • Membrane Proteins / metabolism*
  • Mice
  • Mice, Inbred BALB C
  • Models, Biological
  • Protein Binding
  • Protein Serine-Threonine Kinases / metabolism
  • Receptors, Complement / metabolism*
  • Respiratory Mucosa / pathology
  • Structure-Activity Relationship
  • Time Factors

Substances

  • Aerosols
  • Ligands
  • Membrane Proteins
  • Receptors, Complement
  • complement C3a receptor
  • Arginine
  • Protein Serine-Threonine Kinases