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.
Zacharie
Boulos
B
ProMetic BioSciences Inc, Que, Canada. b.zacharie@prometic.com
Fortin
Daniel
D
Wilb
Nicole
N
Bienvenu
Jean-François
JF
Asselin
Michel
M
Grouix
Brigitte
B
Penney
Christopher
C
D001327:Autoimmune Diseases / Q000188:drug therapy*; D006801:Humans; D007074:Immunoglobulin G / Q000378:metabolism; D018716:Molecular Mimicry; D011687:Purines / Q000138:chemical synthesis* / Q000276:immunology* / Q000627:therapeutic use; D013205:Staphylococcal Protein A / Q000378:metabolism; D013329:Structure-Activity Relationship
D007074:Immunoglobulin G; D011687:Purines; D013205:Staphylococcal Protein A