SYNTHESIS AND ANTIMALARIAL ACTIVITY OF SOME 9-SUBSTITUTED ARTEMISININ DERIVATIVES

被引：38

作者：

ACTON, N

KARLE, JM

MILLER, RE

机构：

[1] Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Washington

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1993年 / 36卷 / 17期

关键词：

D O I：

10.1021/jm00069a014

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several 9-substituted derivatives of the antimalarial drug artemisinin have been prepared by functionalizing the double bond of artemisitene and related compounds. Stereochemical assignments for these compounds were made using a combination of NMR experiments, an X-ray diffraction study of one compound, and chemical correlations of several other compounds with this one compound of unambiguous structure and with its epimer. The compounds synthesized show a wide variation in in vitro antimalarial activity.

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页码：2552 / 2557

页数：6

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