Synthesis of novel 1-hydroxyquinolones with high anti-toxoplasma activity
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. The Japan Institute of Heterocyclic Chemistry.
Tietze, Lutz F.,Ma, Ling
p. 377 - 396
(2011/04/24)
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