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.
N1 - Funding Information:
We thank the NIH (R37 AI 34885), the Johns Hopkins Malaria Research Institute , and the Bloomberg Family Foundation for financial support and Dr. Bryan T. Mott for early participation in this project.
Publisher Copyright:
© 2014 Elsevier Ltd. All rights reserved.
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
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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 -