Synthesis and immunosuppressive effects of novel phthalazine ketone derivatives / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1579-1584, 2013.
Artigo
em Chinês
| WPRIM
| ID: wpr-298041
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.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Farmacologia
/
Ftalazinas
/
Baço
/
Relação Estrutura-Atividade
/
Linfócitos T
/
Química
/
Concentração Inibidora 50
/
Biologia Celular
/
Proliferação de Células
/
Imunossupressores
Limite:
Animais
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2013
Tipo de documento:
Artigo
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