Antimalarial preclinical drug development: A single oral dose of a 5-carbon-linked trioxane dimer plus mefloquine cures malaria-infected mice

Document Type

Journal Article

Publication Date

2-1-2010

Journal

Drug Development Research

Volume

71

Issue

1

DOI

10.1002/ddr.20350

Keywords

Antimalarial chemotherapy; Artemisinin combination therapy (ACT); Single oral dose ACT cure; Trioxane dimers

Abstract

Three new 5-carbon-linked trioxane dimer carboxylate esters have been prepared from the natural trioxane, artemisinin, in only three steps and 40-50% overall yields. Each one of these new chemical entities is at least as efficacious as the clinically used trioxane antimalarial drug artemether when combined with mefloquine hydrochloride in a low single oral dose cure. © 2009 Wiley-Liss, Inc.

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