| 2-烷基取代喹诺酮的合成及生物活性 |
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| 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. |
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| 作者姓名： | 唐元清 吴克美 冯孝章 黄量 |
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| 作者单位： | 中国医学科学院、中国协和医科大学药物研究所 |
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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。
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| 关 键 词： | 喹诺酮生物碱 扩张血管 抗溃疡 合成 |
| 收稿时间： | 1996-11-28 |
Synthesis and bioaction of 2-alkyl-4(1H)-quinolone] |
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| Y Tang,K Wu,X Feng,L Huang.Synthesis and bioaction of 2-alkyl-4(1H)-quinolone][J].Acta Pharmaceutica Sinica,1998,33(2):121-127. |
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| Authors: | Y Tang K Wu X Feng L Huang |
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| Institution: | Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050. |
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| 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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| Keywords: | Quinolone alkaloids Vasorelaxant effect Antiulcer Synthesis |
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