2,6,9-Trisubstituted purine derivatives as protein A mimetics for the treatment of autoimmune diseases

A series of 9-substituted and 2,9-disubstituted 6-(3-aminophenylamino) purines were synthesized and evaluated for their ability to mimic protein A binding to human IgG antibody. The structure–activity relationship (SAR) demonstrates that the 6-(3-aminoanilinyl) purine component was essential for activity. Purine 14 demonstrated significant activity, compared to protein A. These compounds may prove useful for the treatment of autoimmune diseases.

Graphical abstractFirst-in-class series of low molecular weight purine molecules that mimic the ability of protein A to bind to human IgG antibody.Figure optionsDownload full-size imageDownload as PowerPoint slide