摘要
采用两种方法合成了15个2烷基4(1H)喹诺酮生物碱(IVa~g,Va~h),其中5个化合物是从吴茱萸中分离得到的(包括2个新化合物IVa,Vc),IVa,d,f;Vb,c,d,f,h等8个化合物为首次合成。并对所合成的化合物进行了初步药理试验,结果表明具有一定的扩张血管和抗溃疡的作用。IVb还有细胞毒作用。
Five quinolone alkaloids (IVa, Va,c,d,g) including two new compounds (IVa, Vc) from Evodia rutaecarpa and nine analogs are synthesized in good yield by using acidcatalyzed condensation of a series of 3oxoalkkanoic acid esters with aniline and further methylized with methyl iodide. The other analogue Vh is prepared through the reaction of lithium enolate methyl ketone with Nmethylisatoic anhydride. Eight compounds (IVa,d,f; Vb,c,d,f,h) were synthesized for the first time. Pharmacological studies showed that these compounds have vasoconstriction inhibiting and antiulcer effects. Compound IVb also has cytotoxic effect.
出处
《药学学报》
CAS
CSCD
北大核心
1998年第2期121-127,共7页
Acta Pharmaceutica Sinica
关键词
喹诺酮
生物碱
扩张血管
抗溃疡
合成
Quinolone alkaloids
Vasorelaxant effect
Antiulcer
Synthesis