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2-烷基取代喹诺酮的合成及生物活性 被引量:2

SYNTHESIS AND BIOACTION OF 2ALKYL4(1H)QUINOLONE
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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 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.
机构地区 中国医学科学院
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
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  • 1Tang Y Q,Phytochemistry,1996年,43卷,719页 被引量:1

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