N. Acton et al., SYNTHESIS AND ANTIMALARIAL ACTIVITY OF SOME 9-SUBSTITUTED ARTEMISININDERIVATIVES, Journal of medicinal chemistry, 36(17), 1993, pp. 2552-2557
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 diffractio
n study of one compound, and chemical correlations of several other co
mpounds with this one compound of unambiguous structure and with its e
pimer. The compounds synthesized show a wide variation in in vitro ant
imalarial activity.