Spiro and dispiro 1,2,4-trioxolane antimalarials
    8.
    发明授权
    Spiro and dispiro 1,2,4-trioxolane antimalarials 有权
    螺和脱甲基-1,2,4-三恶烷抗疟药

    公开(公告)号:US06486199B1

    公开(公告)日:2002-11-26

    申请号:US09886666

    申请日:2001-06-21

    IPC分类号: A61K31335

    摘要: A means and method for treating malaria using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl or spiropiperidyl ring on the other side of the trioxolane group, whereby the spirocyclohexyl ring is preferably functionalized or substituted at the 4-position or a spiropiperidyl ring that is functionalized or substituted at the nitrogen atom. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.

    摘要翻译: 描述了使用螺或二脱氧-1,2,4-三恶烷处理疟疾的方法和方法。 优选的1,2,4-三氧杂环戊烷包括在三氧杂环戊烷基一侧的双金刚烷基,三氧杂环戊烷基的另一侧上的螺环己基或螺哌啶环,其中螺环己基环优选在4位官能化或取代 或在氮原子上被官能化或取代的螺哌啶基环。 与青蒿素半合成衍生物相比,本发明的化合物在结构上简单,易于合成,无毒,对抗疟疾寄生虫有效。