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几种氟化青蒿素衍生物的合成及其抗疟活性

Synthesis and antimalarial activities of several fluorinated artemisinin derivatives.

作者信息

Pu Y M, Torok D S, Ziffer H, Pan X Q, Meshnick S R

机构信息

Laboratory of Chemical Physics, NIDDK, Bethesda, Maryland 20892-0510, USA.

出版信息

J Med Chem. 1995 Sep 29;38(20):4120-4. doi: 10.1021/jm00020a028.

Abstract

The carbonyl groups in several artemisinin derivatives were converted into geminal difluorinated compounds on treatment with diethylaminosulfur trifluoride. A number of other mono- and polyfluorinated artemisinin derivatives were prepared. Their in vitro antimalarial activities were all equal to or greater than the nonfluorinated analogs or precursors.

摘要

几种青蒿素衍生物中的羰基在与二乙氨基三氟化硫反应时被转化为偕二氟代化合物。制备了许多其他单氟和多氟青蒿素衍生物。它们的体外抗疟活性均等于或高于未氟化的类似物或前体。

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