Antimalarial chemotherapy: Orally curative artemisinin-derived trioxane dimer esters

Ryan C. Conyers, Jennifer R. Mazzone, Abhai K. Tripathi, David J. Sullivan, Gary H. Posner

Research output: Contribution to journalArticle

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 6 mg/kg combined with 18 mg/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.

Original languageEnglish (US)
Pages (from-to)245-248
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume25
Issue number2
DOIs
StatePublished - Jan 15 2015

Keywords

  • Antimalarial chemotherapy
  • Oral bioavailability
  • Single oral dose ACT
  • Trioxane dimer esters

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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