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

doi:10.1016/j.bmcl.2010.09.123

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

Bloomberg School of Public Health

Research output: Contribution to journal › Article › peer-review

17 Scopus citations

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 language	English (US)
Pages (from-to)	2773-2775
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	21
Issue number	9
DOIs	https://doi.org/10.1016/j.bmcl.2010.09.123
State	Published - 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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10.1016/j.bmcl.2010.09.123

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

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.",

keywords = "Antimalarial chemotherapy, Single oral dose ACT cure, Trioxane dimer orthoesters",

author = "Moon, {Deuk Kyu} and Abhai Tripathi and David Sullivan and Siegler, {Maxime A.} and Sean Parkin and Posner, {Gary H.}",

note = "Funding Information: We thank the NIH ( AI 34885 to G.H.P.), the Johns Hopkins Malaria Research Institute , and the Bloomberg Family Foundation for financial support (to G.H.P. and to D.S.). ",

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AU - Tripathi, Abhai

AU - Sullivan, David

AU - Siegler, Maxime A.

AU - Parkin, Sean

AU - Posner, Gary H.

N1 - Funding Information: We thank the NIH ( AI 34885 to G.H.P.), the Johns Hopkins Malaria Research Institute , and the Bloomberg Family Foundation for financial support (to G.H.P. and to D.S.).

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

Abstract

Keywords

ASJC Scopus subject areas

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