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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

O'Neill, P. M., Rawe, S. L., Borstnik, K., Miller, A., Ward, Stephen ORCID: https://orcid.org/0000-0003-2331-3192, Bray, Patrick, Davies, Jill, Oh, C. H. and Posner, G. H. (2005) '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'. Chembiochem, Vol 6, Issue 11, pp. 2048-2054.

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Abstract

The aim of this study was to synthesise pure enantiomers of potent antimalarial I,2,4-trioxanes, which are related to the natural antimalarial ortemisinin, 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 (+)-7a, (-)-7a and (+)-7b, (-)-7b, showed the some level of in vitro antiparasitic activity.

Item Type: Article
Uncontrolled Keywords: artemisinin asymmetric synthesis chirality drug design medicinal chemistry qinghaosu artemisinin drug artemisinin invitro activity endoperoxides derivatives 3-aryltrioxanes chloroquine alkylation trioxanes analogs
Subjects: QV Pharmacology > Anti-Inflammatory Agents. Anti-Infective Agents. Antineoplastic Agents > QV 256 Antimalarials
QX Parasitology > Protozoa > QX 135 Plasmodia
Faculty: Department: Groups (2002 - 2012) > Molecular & Biochemical Parasitology Group
Digital Object Identifer (DOI): https://doi.org/10.1002/cbic.200500048
Depositing User: Ms Julia Martin
Date Deposited: 29 Jul 2011 14:28
Last Modified: 06 Feb 2018 13:02
URI: http://archive.lstmed.ac.uk/id/eprint/1866

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