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

Chemistry

Producción científica: Article › revisión exhaustiva

23 Citas (Scopus)

Resumen

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.

Idioma original	English
Páginas (desde-hasta)	2773-2775
Número de páginas	3
Publicación	Bioorganic and Medicinal Chemistry Letters
Volumen	21
N.º	9
DOI	https://doi.org/10.1016/j.bmcl.2010.09.123
Estado	Published - may 1 2011

Nota bibliográfica

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.).

Financiación

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.).

Financiadores	Número del financiador
National Institutes of Health (NIH)
National Institute of Allergy and Infectious F32-AI286447 Cydney N. Johnson Diseases National Institute of Allergy and Infectious R01AI168214 Jason W. Rosch Diseases National Institute of Allergy and Infectious P30 Cydney N. Johnson Diseases National Institute of Allergy and Infectious R00-AI166116 Christopher D. Radka Diseases National Institute of Allergy and Infectious T32-AI106700 Cydney N. Johnson Diseases National Institute of Allergy and Infectious R01AI192221 Jason W. Rosch Diseases National Inst...	R37AI034885
Bloomberg Family Foundation
Johns Hopkins Malaria Research Institute, Johns Hopkins Bloomberg School of Public Health

ODS de las Naciones Unidas

Este resultado contribuye a los siguientes Objetivos de Desarrollo Sostenible

Good health and well being

ASJC Scopus subject areas

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

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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.",

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

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AU - Tripathi, Abhai

AU - Sullivan, David

AU - Siegler, Maxime A.

AU - Parkin, Sean

AU - Posner, Gary H.

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

Resumen

Nota bibliográfica

Financiación

ODS de las Naciones Unidas

ASJC Scopus subject areas

Acceder al documento

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Huella

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