Résumé
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.
Sujets)
Animaux , Femelle , Souris , Prolifération cellulaire , IMP dehydrogenase , Métabolisme , Immunosuppresseurs , Chimie , Pharmacologie , Concentration inhibitrice 50 , Souris de lignée BALB C , Phtalazines , Chimie , Pharmacologie , Rate , Biologie cellulaire , Relation structure-activité , Lymphocytes TRésumé
<p><b>OBJECTIVE</b>To investigate the chemical constituents of Potentilla chinensis.</p><p><b>METHOD</b>Silica gel column chromatography and Sephadex LH - 20 gel column chromatography were employed for the isolation and purfication. The structures were identified on the basis of spectral data and chemical evidence.</p><p><b>RESULT</b>Six compounds were isolated and identified as follows: 3-hydroxy-11-ursen-28, 13-olide, 11, 12-dehydroursolic acid lactone (1), 3-O-acetyl pomolic acid (2), betulinic acid (3), 3-oxo-12-ursen-28-oic acid (4), ursolic acid (5), oleanic acid (6). CONCLOUSION: All these compounds were isolated from P. chinensis for the first time, compound 1, 2, 4 were isolated from this genus for the first time.</p>