Synthesis and biological evaluation of novel lipid A antagonists

A mimetic of Lipid A with a β-N(OMe) glycosidic linkage, four linear C-14 hydrophobic chains and without phosphate groups has been prepared together with its β-O-linked analogue. Both these molecules were active in inhibiting the inflammatory action of Escherichia coli lipid A on MT2 macrophages in a dose-dependent manner, while they were completely devoid of inflammatory activity.

A novel lipid A mimetic with a methoxyamino glycosidic linkage presents antagonist activity against bacterial LPS.Figure optionsDownload as PowerPoint slide