Toll-like receptor 2 antagonists. Part 1: preliminary SAR investigation of novel synthetic phospholipids

Bioorg Med Chem Lett. 2005 Dec 15;15(24):5494-8. doi: 10.1016/j.bmcl.2005.08.080. Epub 2005 Oct 19.

Abstract

Novel synthetic phospholipid compound 1 was discovered to be an antagonist of human toll-like receptor 2 (TLR2) signaling. In a preliminary SAR campaign we synthesized several analogues of 1 and found that considerable structural changes could be made without loss of TLR2 antagonistic activity.

MeSH terms

  • Humans
  • Indicators and Reagents
  • Kinetics
  • Models, Molecular
  • Phospholipids / chemical synthesis*
  • Phospholipids / pharmacology*
  • Stereoisomerism
  • Structure-Activity Relationship
  • Toll-Like Receptor 2 / antagonists & inhibitors*

Substances

  • Indicators and Reagents
  • Phospholipids
  • Toll-Like Receptor 2