A series of phthalazine ketone compounds were synthesized and the structures were confirmed by H NMR and HR-MS spectrum. All target compounds were obtained through 7 steps, including selective reduction, nitration, bromination, ring enlargement, reduction, Knoevenagel and acylated reaction. The compounds were evaluated for their immunosuppressive effects of T-cell proliferation and inhibitory activity of IMPDH type II in vitro, as well as their structure-activity relationship were assessed. Several compounds exhibited strong immunosuppressive properties, especially compounds 7f and 7h, with IC50 values of 0.093 micromol x L(-1) and 0.14 micromol x L(-1) respectively, which were superior to mycophenolic acid. The information obtained from the studies may be useful for further research on the immunosuppressive agents.

Animals ; Carbon Tetrachloride ; Collagen Type IV ; blood ; Disease Models, Animal ; Hyaluronic Acid ; blood ; Inflammation ; drug therapy ; etiology ; Interferon-alpha ; therapeutic use ; Laminin ; blood ; Liver Cirrhosis ; blood ; chemically induced ; complications ; drug therapy ; pathology ; Rats ; Rats, Sprague-Dawley ; Transforming Growth Factor beta ; blood

Adolescent ; Adult ; Alanine Transaminase ; blood ; DNA, Viral ; analysis ; Female ; Hepatitis B Surface Antigens ; blood ; Hepatitis B e Antigens ; blood ; Hepatitis B, Chronic ; blood ; drug therapy ; Humans ; Interferon Type I ; therapeutic use ; Interferon-alpha ; therapeutic use ; Liver Function Tests ; Male ; Middle Aged ; Recombinant Proteins ; Treatment Outcome

0.05 ), However, all pasameters showed significantly milder or lower in interferon ? treated group than incontrol group at the 6th, 12th week( P