A dermatan sulfate (DS) repeating disaccharide analog, α-l-idopyranosiduronate-(1→3)-2-amino-2-deoxy-4,6-di-O-sulfo-β-d-galactopyranoside, has been convergently synthesized and successfully applied to prepare the GAG-functionalized gold glyconanoparticle. This new material exhibited good anti-inflammatory activity which was comparable to that of the drug ibuprofen incarrageenan-induced paw edema in a rat model.