A single, low, oral dose of a 5-carbon-linked trioxane dimer orthoester plus mefloquine cures malaria-infected mice

Deuk Kyu Moon, Abhai Tripathi, David Sullivan, Maxime A. Siegler, Sean Parkin, Gary H. Posner

Research output: Contribution to journalArticle

Abstract

Four 5-carbon-linked trioxane dimer orthoesters (6a-6d) have been prepared in 4 or 5 chemical steps from the natural trioxane artemisinin (1). When administered orally to malaria-infected mice using a single dose of only 6 mg/kg body weight along with 18 mg/kg of mefloquine hydrochloride, trioxane dimer orthoester sulfone 6d completely and safely cured the mice; after 30 days, the cured mice showed no detectable parasitemia, gained at least as much weight as the control mice (no infection), and behaved normally.

Original languageEnglish (US)
Pages (from-to)2773-2775
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number9
DOIs
StatePublished - May 1 2011

Keywords

  • Antimalarial chemotherapy
  • Single oral dose ACT cure
  • Trioxane dimer orthoesters

ASJC Scopus subject areas

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

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