Antimalarial chemotherapy: Orally curative artemisinin-derived trioxane dimer esters

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

doi:10.1016/j.bmcl.2014.11.064

Antimalarial chemotherapy: Orally curative artemisinin-derived trioxane dimer esters

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

Bloomberg School of Public Health

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

11 Scopus citations

Abstract

Eight new artemisinin-derived trioxane dimer esters 5 have been prepared and tested for antimalarial efficacy in malaria-infected mice. At a single oral dose of only 6 mg/kg combined with 18 mg/kg of mefloquine, each of the dimer esters 5 outperformed the antimalarial drug artemether (2). The most efficacious dimer, dichlorobenzoate ester 5h, prolonged mouse survival past day 30 of infection with three of the four mice in this group having no detectable parasitemia and appearing and acting healthy on day 30.

Original language	English (US)
Pages (from-to)	245-248
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	25
Issue number	2
DOIs	https://doi.org/10.1016/j.bmcl.2014.11.064
State	Published - Jan 15 2015

Keywords

Antimalarial chemotherapy
Oral bioavailability
Single oral dose ACT
Trioxane dimer esters

ASJC Scopus subject areas

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

Access to Document

10.1016/j.bmcl.2014.11.064

Cite this

@article{b803f81c67384e30bfcee8d1ce246c30,

title = "Antimalarial chemotherapy: Orally curative artemisinin-derived trioxane dimer esters",

abstract = "Eight new artemisinin-derived trioxane dimer esters 5 have been prepared and tested for antimalarial efficacy in malaria-infected mice. At a single oral dose of only 6 mg/kg combined with 18 mg/kg of mefloquine, each of the dimer esters 5 outperformed the antimalarial drug artemether (2). The most efficacious dimer, dichlorobenzoate ester 5h, prolonged mouse survival past day 30 of infection with three of the four mice in this group having no detectable parasitemia and appearing and acting healthy on day 30.",

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

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

year = "2015",

month = jan,

day = "15",

doi = "10.1016/j.bmcl.2014.11.064",

language = "English (US)",

volume = "25",

pages = "245--248",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd",

number = "2",

}

TY - JOUR

T1 - Antimalarial chemotherapy

T2 - Orally curative artemisinin-derived trioxane dimer esters

AU - Conyers, Ryan C.

AU - Mazzone, Jennifer R.

AU - Tripathi, Abhai K.

AU - Sullivan, David J.

AU - Posner, Gary H.

PY - 2015/1/15

Y1 - 2015/1/15

N2 - Eight new artemisinin-derived trioxane dimer esters 5 have been prepared and tested for antimalarial efficacy in malaria-infected mice. At a single oral dose of only 6 mg/kg combined with 18 mg/kg of mefloquine, each of the dimer esters 5 outperformed the antimalarial drug artemether (2). The most efficacious dimer, dichlorobenzoate ester 5h, prolonged mouse survival past day 30 of infection with three of the four mice in this group having no detectable parasitemia and appearing and acting healthy on day 30.

AB - Eight new artemisinin-derived trioxane dimer esters 5 have been prepared and tested for antimalarial efficacy in malaria-infected mice. At a single oral dose of only 6 mg/kg combined with 18 mg/kg of mefloquine, each of the dimer esters 5 outperformed the antimalarial drug artemether (2). The most efficacious dimer, dichlorobenzoate ester 5h, prolonged mouse survival past day 30 of infection with three of the four mice in this group having no detectable parasitemia and appearing and acting healthy on day 30.

KW - Antimalarial chemotherapy

KW - Oral bioavailability

KW - Single oral dose ACT

KW - Trioxane dimer esters

UR - http://www.scopus.com/inward/record.url?scp=84949129360&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84949129360&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2014.11.064

DO - 10.1016/j.bmcl.2014.11.064

M3 - Article

C2 - 25481079

AN - SCOPUS:84949129360

SN - 0960-894X

VL - 25

SP - 245

EP - 248

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 2

ER -

Antimalarial chemotherapy: Orally curative artemisinin-derived trioxane dimer esters

Abstract

Keywords

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this