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Antimalarial preclinical drug development: a single oral dose of a 5‐carbon‐linked trioxane dimer plus mefloquine cures malaria‐infected mice
Author(s) -
Moon Deuk Kyu,
Singhal Vandana,
Kumar Nirbhay,
Shapiro Theresa A.,
Posner Gary H.
Publication year - 2010
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.20350
Subject(s) - trioxane , mefloquine , artemisinin , pharmacology , dimer , drug , chemistry , malaria , antimalarial agent , artemether , hydrochloride , oral administration , medicine , chloroquine , plasmodium falciparum , organic chemistry , immunology , copolymer , polymer
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. Drug Dev Res 71: 76–81, 2010. © 2009 Wiley‐Liss, Inc.