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Antimalarial chemotherapy: orally curative artemisinin-derived trioxane dimer esters.

Authors :
Conyers RC
Mazzone JR
Tripathi AK
Sullivan DJ
Posner GH
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2015 Jan 15; Vol. 25 (2), pp. 245-8. Date of Electronic Publication: 2014 Nov 27.
Publication Year :
2015

Abstract

Eight new artemisinin-derived trioxane dimer esters 5 have been prepared and tested for antimalarial efficacy in malaria-infected mice. At a single oral dose of only 6mg/kg combined with 18mg/kg of mefloquine, each of the dimer esters 5 outperformed the antimalarial drug artemether (2). The most efficacious dimer, dichlorobenzoate ester 5h, prolonged mouse survival past day 30 of infection with three of the four mice in this group having no detectable parasitemia and appearing and acting healthy on day 30.<br /> (Copyright © 2014 Elsevier Ltd. All rights reserved.)

Details

Language :
English
ISSN :
1464-3405
Volume :
25
Issue :
2
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
25481079
Full Text :
https://doi.org/10.1016/j.bmcl.2014.11.064