title: Antimalarial chemotherapy: orally curative artemisinin-derived trioxane dimer esters.
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.
authors.affiliation: Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 North Charles Street, Baltimore, MD 21218, United States.
authors.forename: Ryan C
authors.initials: RC
authors.lastname: Conyers
authors.affiliation: Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 North Charles Street, Baltimore, MD 21218, United States.
authors.forename: Jennifer R
authors.initials: JR
authors.lastname: Mazzone
authors.affiliation: W. Harry Feinstone, Department of Molecular Microbiology and Immunology, Bloomberg School of Public Health, The Johns Hopkins University, Baltimore, MD 21205, United States; The Johns Hopkins Malaria Research Institute, Bloomberg School of Public Health, The Johns Hopkins University, Baltimore, MD 21205, United States.
authors.forename: Abhai K
authors.initials: AK
authors.lastname: Tripathi
authors.affiliation: W. Harry Feinstone, Department of Molecular Microbiology and Immunology, Bloomberg School of Public Health, The Johns Hopkins University, Baltimore, MD 21205, United States; The Johns Hopkins Malaria Research Institute, Bloomberg School of Public Health, The Johns Hopkins University, Baltimore, MD 21205, United States.
authors.forename: David J
authors.initials: DJ
authors.lastname: Sullivan
authors.affiliation: Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 North Charles Street, Baltimore, MD 21218, United States; The Johns Hopkins Malaria Research Institute, Bloomberg School of Public Health, The Johns Hopkins University, Baltimore, MD 21205, United States. Electronic address: ghp@jhu.edu.
authors.forename: Gary H
authors.initials: GH
authors.lastname: Posner
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000962:Antimalarials / Q000008:administration & dosage* / Q000737:chemistry*; D037621:Artemisinins / Q000008:administration & dosage* / Q000737:chemistry*; D019281:Dimerization; D008288:Malaria / Q000188:drug therapy*; D051379:Mice; D010962:Plasmodium berghei / Q000187:drug effects*
chemical_list: D000962:Antimalarials; D037621:Artemisinins; C031327:artemisinin
keywords: Antimalarial chemotherapy; Oral bioavailability; Single oral dose ACT; Trioxane dimer esters