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

Phospholipid compound 1 was discovered as a novel antagonist of toll-like receptor 2 signaling. Synthesis and biological properties are described for 1 and eight related analogues. 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.