Malaria-infected mice are cured by a single low dose of a new silylamide trioxane plus mefloquine

Lauren E. Woodard; Bryan T. Mott; Vandana Singhal; Nirbhay Kumar; Theresa A. Shapiro; Gary H. Posner

doi:10.3390/ph2030228

Malaria-infected mice are cured by a single low dose of a new silylamide trioxane plus mefloquine

Lauren E. Woodard, Bryan T. Mott, Vandana Singhal, Nirbhay Kumar, Theresa A. Shapiro, Gary H. Posner

School of Medicine

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

Abstract

Three thermally and hydrolytically stable silylamide trioxanes have been prepared from the natural trioxane artemisinin in only five simple chemical steps and in at least 56% overall yield. Two of these new chemical entities completely cured malaria-infected mice at a single oral dose of only 8 mg/kg combined with 24 mg/kg of mefloquine hydrochloride. The high efficacy of this ACT chemotherapy is considerably better than the efficacy using the popular trioxane drug artemether plus mefloquine hydrochloride.

Original language	English (US)
Pages (from-to)	228-235
Number of pages	8
Journal	Pharmaceuticals
Volume	2
Issue number	3
DOIs	https://doi.org/10.3390/ph2030228
State	Published - Dec 2009

Keywords

Antimalarial monomers and dimmers
Silylamide trioxanes
Single dose oral cure

ASJC Scopus subject areas

Molecular Medicine
Pharmaceutical Science
Drug Discovery

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10.3390/ph2030228

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abstract = "Three thermally and hydrolytically stable silylamide trioxanes have been prepared from the natural trioxane artemisinin in only five simple chemical steps and in at least 56% overall yield. Two of these new chemical entities completely cured malaria-infected mice at a single oral dose of only 8 mg/kg combined with 24 mg/kg of mefloquine hydrochloride. The high efficacy of this ACT chemotherapy is considerably better than the efficacy using the popular trioxane drug artemether plus mefloquine hydrochloride.",

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author = "Woodard, {Lauren E.} and Mott, {Bryan T.} and Vandana Singhal and Nirbhay Kumar and Shapiro, {Theresa A.} and Posner, {Gary H.}",

note = "Funding Information: We thank the NIH (AI 34885 to GHP), the Johns Hopkins Malaria Research Institute and the Bloomberg Family Foundation for financial support (to GHP and to NK). Publisher Copyright: {\textcopyright} 2009 by the authors; licensee Molecular Diversity Preservation International, Basel, Switzerland.",

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AU - Mott, Bryan T.

AU - Singhal, Vandana

AU - Kumar, Nirbhay

AU - Shapiro, Theresa A.

AU - Posner, Gary H.

N1 - Funding Information: We thank the NIH (AI 34885 to GHP), the Johns Hopkins Malaria Research Institute and the Bloomberg Family Foundation for financial support (to GHP and to NK). Publisher Copyright: © 2009 by the authors; licensee Molecular Diversity Preservation International, Basel, Switzerland.

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N2 - Three thermally and hydrolytically stable silylamide trioxanes have been prepared from the natural trioxane artemisinin in only five simple chemical steps and in at least 56% overall yield. Two of these new chemical entities completely cured malaria-infected mice at a single oral dose of only 8 mg/kg combined with 24 mg/kg of mefloquine hydrochloride. The high efficacy of this ACT chemotherapy is considerably better than the efficacy using the popular trioxane drug artemether plus mefloquine hydrochloride.

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Malaria-infected mice are cured by a single low dose of a new silylamide trioxane plus mefloquine

Abstract

Keywords

ASJC Scopus subject areas

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