Synthesis and immunosuppressive effects of novel phthalazine ketone derivatives.
- Author:
Yali WANG
;
Qinghe WANG
;
Hongguang YANG
;
Bojun HAO
;
Guodong LIANG
;
Chongguo JIANG
;
Maosheng CHENG
- Publication Type:Journal Article
- From:
Acta Pharmaceutica Sinica
2013;48(10):1579-84
- CountryChina
- Language:Chinese
-
Abstract:
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.
