唐元清, 吴克美, 冯孝章, 黄量. 2-烷基取代喹诺酮的合成及生物活性J. 药学学报, 1998, 33(2): 121-127.
引用本文: 唐元清, 吴克美, 冯孝章, 黄量. 2-烷基取代喹诺酮的合成及生物活性J. 药学学报, 1998, 33(2): 121-127.
Tang Yuanqing, Wu Kemei Feng Xiaozhang , Huang Liang, . SYNTHESIS AND BIOACTION OF 2ALKYL4(1H)QUINOLONEJ. Acta Pharmaceutica Sinica, 1998, 33(2): 121-127.
Citation: Tang Yuanqing, Wu Kemei Feng Xiaozhang , Huang Liang, . SYNTHESIS AND BIOACTION OF 2ALKYL4(1H)QUINOLONEJ. Acta Pharmaceutica Sinica, 1998, 33(2): 121-127.

2-烷基取代喹诺酮的合成及生物活性

SYNTHESIS AND BIOACTION OF 2ALKYL4(1H)QUINOLONE

  • 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。

     

    Abstract: 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 acidcatalyzed condensation of a series of 3oxoalkkanoic 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 nmethylisatoic 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.

     

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