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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.
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: | 17 Jul 2020 10:57 |
| URI: | https://archive.lstmed.ac.uk/id/eprint/1866 |
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