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

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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.

Graphical abstract

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.

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Acknowledgments

We thank Donna Young, Minglun Wang, Kara Loiacono, and Melinda Genest for developing and running the biological assays.

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