Antimalarial chemotherapy: Artemisinin-derived dimer carbonates and thiocarbonates

Jennifer R. Mazzone; Ryan C. Conyers; Abhai K. Tripathi; David J. Sullivan; Gary H. Posner

doi:10.1016/j.bmcl.2014.04.025

Antimalarial chemotherapy: Artemisinin-derived dimer carbonates and thiocarbonates

Jennifer R. Mazzone, Ryan C. Conyers, Abhai K. Tripathi, David J. Sullivan, Gary H. Posner

Bloomberg School of Public Health

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

15 Scopus citations

Abstract

Several 2-carbon-linked trioxane dimer secondary alcohol carbonates 14 and thiocarbonates 15, combined with mefloquine and administered in a low single oral dose, prolonged the survival times of malaria-infected mice much more effectively than the popular monomeric antimalarial drug artemether plus mefloquine. Three dimer carbonates 14 and one dimer thiocarbonate 15 partially cured malaria-infected mice.

Original language	English (US)
Pages (from-to)	2440-2443
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	24
Issue number	11
DOIs	https://doi.org/10.1016/j.bmcl.2014.04.025
State	Published - Jun 1 2014

Keywords

Antimalarial chemotherapy
Oral bioavailability
Single oral dose ACT
Trioxane dimers

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.2014.04.025

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title = "Antimalarial chemotherapy: Artemisinin-derived dimer carbonates and thiocarbonates",

abstract = "Several 2-carbon-linked trioxane dimer secondary alcohol carbonates 14 and thiocarbonates 15, combined with mefloquine and administered in a low single oral dose, prolonged the survival times of malaria-infected mice much more effectively than the popular monomeric antimalarial drug artemether plus mefloquine. Three dimer carbonates 14 and one dimer thiocarbonate 15 partially cured malaria-infected mice.",

keywords = "Antimalarial chemotherapy, Oral bioavailability, Single oral dose ACT, Trioxane dimers",

author = "Mazzone, {Jennifer R.} and Conyers, {Ryan C.} and Tripathi, {Abhai K.} and Sullivan, {David J.} and Posner, {Gary H.}",

note = "Funding Information: We thank NIH (Grant R37 AI 34885 to G.H.P.), The Johns Hopkins Malaria Research Institute , and the Bloomberg Family Foundation for financial support. ",

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T2 - Artemisinin-derived dimer carbonates and thiocarbonates

AU - Mazzone, Jennifer R.

AU - Conyers, Ryan C.

AU - Tripathi, Abhai K.

AU - Sullivan, David J.

AU - Posner, Gary H.

N1 - Funding Information: We thank NIH (Grant R37 AI 34885 to G.H.P.), The Johns Hopkins Malaria Research Institute , and the Bloomberg Family Foundation for financial support.

PY - 2014/6/1

Y1 - 2014/6/1

N2 - Several 2-carbon-linked trioxane dimer secondary alcohol carbonates 14 and thiocarbonates 15, combined with mefloquine and administered in a low single oral dose, prolonged the survival times of malaria-infected mice much more effectively than the popular monomeric antimalarial drug artemether plus mefloquine. Three dimer carbonates 14 and one dimer thiocarbonate 15 partially cured malaria-infected mice.

AB - Several 2-carbon-linked trioxane dimer secondary alcohol carbonates 14 and thiocarbonates 15, combined with mefloquine and administered in a low single oral dose, prolonged the survival times of malaria-infected mice much more effectively than the popular monomeric antimalarial drug artemether plus mefloquine. Three dimer carbonates 14 and one dimer thiocarbonate 15 partially cured malaria-infected mice.

KW - Antimalarial chemotherapy

KW - Oral bioavailability

KW - Single oral dose ACT

KW - Trioxane dimers

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Antimalarial chemotherapy: Artemisinin-derived dimer carbonates and thiocarbonates

Abstract

Keywords

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