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Malaria-Infected Mice Are Cured by a Single Low Dose of a New Silylamide Trioxane Plus Mefloquine
Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 North Charles Street, Baltimore, Maryland 21218-2685, MD, USA
Department of Molecular Microbiology and Immunology, Malaria Research Institute, Johns Hopkins Bloomberg School of Public Health, Baltimore, MD Baltimore, MD 21205, USA
Division of Clinical Pharmacology, Department of Medicine, School of Medicine, The Johns Hopkins University, Baltimore, MD 21205, USA
* Author to whom correspondence should be addressed.
Received: 24 November 2009; in revised form: 8 December 2009 / Accepted: 18 December 2009 / Published: 21 December 2009
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 malariainfected 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.
Keywords: silylamide trioxanes; antimalarial monomers and dimmers; single dose oral cure
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MDPI and ACS Style
Woodard, L.E.; Mott, B.T.; Singhal, V.; Kumar, N.; Shapiro, T.A.; Posner, G.H. Malaria-Infected Mice Are Cured by a Single Low Dose of a New Silylamide Trioxane Plus Mefloquine. Pharmaceuticals 2009, 2, 228-235.
Woodard LE, Mott BT, Singhal V, Kumar N, Shapiro TA, Posner GH. Malaria-Infected Mice Are Cured by a Single Low Dose of a New Silylamide Trioxane Plus Mefloquine. Pharmaceuticals. 2009; 2(3):228-235.
Woodard, Lauren E.; Mott, Bryan T.; Singhal, Vandana; Kumar, Nirbhay; Shapiro, Theresa A.; Posner, Gary H. 2009. "Malaria-Infected Mice Are Cured by a Single Low Dose of a New Silylamide Trioxane Plus Mefloquine." Pharmaceuticals 2, no. 3: 228-235.