Synthesis of novel 1-hydroxyquinolones with high anti-toxoplasma activity
Synthesis of novel 1-hydroxyquinolones with high anti-toxoplasma activity
复制标题
DOI：
10.3987/com-10-s(e)9
复制
发表时间：
2010-12
期刊：
影响因子：
0.6
通讯作者：
L. Tietze;Ling Ma
中科院分区：
文献类型：
--
作者：
L. Tietze;Ling Ma
分别以苯胺和羟基苯胺为原料，与β-酮酯10a-c反应，合成了新的羟基喹诺酮类化合物2-5，用于治疗疟疾和弓形虫病。作为产物，分别获得喹诺酮8和15。然后进行苄基化、氧化和氢化，得到所需的物质。化合物2具有与批准的药物阿托伐醌类似的抗疟疾活性。
All for the treatment of malaria and toxoplasmosis the novel hydroxyquinolones 2-5 were prepared by reaction of aniline and hydroxyaniline, respectively and the β-ketoesters 10a-c. As products the quinolones 8 and 15, respectively were obtained. Benzylation, oxidation and hydrogenation then led to the desired substances. Compound 2 has a similar anti-malaria activity as the approved drug Atovaquone.