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Start Over Author "Borstnik, Kristina" Journal chembiochem a european journal of chemical biology

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1 results on '"Borstnik, Kristina"'

1. Enantiomeric 1,2,4-trioxanes display equivalent in vitro antimalarial activity versus Plasmodium falciparum malaria parasites: implications for the molecular mechanism of action of the artemisinins.

Author

O'Neill PM, Rawe SL, Borstnik K, Miller A, Ward SA, Bray PG, Davies J, Oh CH, and Posner GH

Subjects
Animals, Antimalarials chemical synthesis, Antimalarials chemistry, Artemisinins metabolism, Drug Design, Heterocyclic Compounds chemical synthesis, Heterocyclic Compounds chemistry, Inhibitory Concentration 50, Molecular Structure, Parasitic Sensitivity Tests, Stereoisomerism, Antimalarials pharmacology, Artemisinins pharmacology, Heterocyclic Compounds pharmacology, Plasmodium falciparum drug effects
Abstract

The aim of this study was to synthesise pure enantiomers of potent antimalarial 1,2,4-trioxanes, which are related to the natural antimalarial artemisinin, and then to assay each against a panel of Plasmodium falciparum strains. The working hypothesis was that if the artemisinin derivatives interact with a specific protein-target site, then there should be stereoselective differences in their activity. In five different P. falciparum isolates, however, the trioxane enantiomers (+)-7 a, (-)-7 a and (+)-7 b, (-)-7 b, showed the same level of in vitro antiparasitic activity.

Published
2005
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