Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4026-30. doi: 10.1016/j.bmcl.2009.06.027. Epub 2009 Jun 13.


We reported recently the Structure-Activity Relationship (SAR) of a class of CXCL8 allosteric modulators. They invariably share a 2-arylpropionic moiety so far considered a key structural determinant of the biological activity. We show the results of recent SAR studies on a novel series of phenylacetic derivatives supported by a combined approach of mutagenesis experiments and conformational analysis. The results suggest novel insights on the fine role of the propionic/acetic chain in the modulation of CXCL8 receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Allosteric Regulation
  • Allosteric Site
  • Chemistry, Organic / methods
  • Chemistry, Pharmaceutical / methods
  • Chemotaxis
  • Humans
  • Inhibitory Concentration 50
  • Models, Chemical
  • Models, Molecular
  • Molecular Conformation
  • Mutagenesis
  • Mutation
  • Receptors, Interleukin-8A / antagonists & inhibitors*
  • Structure-Activity Relationship


  • Receptors, Interleukin-8A