Literature DB >> 25481079

Antimalarial chemotherapy: orally curative artemisinin-derived trioxane dimer esters.

Ryan C Conyers1, Jennifer R Mazzone1, Abhai K Tripathi2, David J Sullivan2, Gary H Posner3.   

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 6mg/kg combined with 18mg/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.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Antimalarial chemotherapy; Oral bioavailability; Single oral dose ACT; Trioxane dimer esters

Mesh：

Substances：

Year:  2014        PMID： 25481079      PMCID： PMC4277730          DOI： 10.1016/j.bmcl.2014.11.064

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  42 in total

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3.  Orally active esters of dihydroartemisinin: Synthesis and antimalarial activity against multidrug-resistant Plasmodium yoelii in mice.

Authors:  Chandan Singh; Sandeep Chaudhary; Sunil K Puri
Journal:  Bioorg Med Chem Lett       Date:  2008-01-05       Impact factor: 2.823

4.  Design, synthesis and evaluation of new tricyclic endoperoxides as potential antiplasmodial agents.

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5.  Bile acid-based 1,2,4-trioxanes: synthesis and antimalarial assessment.

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Review 10.  Progress in the research of artemisinin-related antimalarials: an update.

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2.  Artemisinin-(Iso)quinoline Hybrids by C-H Activation and Click Chemistry: Combating Multidrug-Resistant Malaria.

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