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. 1993 Aug 20;36(17):2552-7.
doi: 10.1021/jm00069a014.

Synthesis and antimalarial activity of some 9-substituted artemisinin derivatives

N Acton  1 , J M Karle, R E Miller
Affiliations

Synthesis and antimalarial activity of some 9-substituted artemisinin derivatives

N Acton et al. J Med Chem. .

Abstract

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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