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

Mark R Spyvee; Huiming Zhang; Lynn D Hawkins; Jesse C Chow

doi:10.1016/j.bmcl.2005.08.080

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.

Authors

Mark R Spyvee¹, Huiming Zhang, Lynn D Hawkins, Jesse C Chow

Affiliation

¹ Lead Optimization Department, Eisai Research Institute, 100 Research Drive, Wilmington, MA 01887, USA. [email protected]

PMID: 16236498
DOI: 10.1016/j.bmcl.2005.08.080

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