Toll-like receptor 2 antagonists. Part 1: preliminary SAR investigation of novel synthetic phospholipids.
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.
Spyvee
Mark R
MR
Lead Optimization Department, Eisai Research Institute, 100 Research Drive, Wilmington, MA 01887, USA. mark_spyvee@eisai.com
Zhang
Huiming
H
Hawkins
Lynn D
LD
Chow
Jesse C
JC
D006801:Humans; D007202:Indicators and Reagents; D007700:Kinetics; D008958:Models, Molecular; D010743:Phospholipids / Q000138:chemical synthesis* / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D051195:Toll-Like Receptor 2 / Q000037:antagonists & inhibitors*
D007202:Indicators and Reagents; D010743:Phospholipids; D051195:Toll-Like Receptor 2