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Issue 28, 2014
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Design, synthesis and evaluation of new tricyclic endoperoxides as potential antiplasmodial agents

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Abstract

Diastereoselective autoxidation allowed preparation of new tricyclic endoperoxides. These compounds and their methylated analogs were evaluated against the in vitro growth of Plasmodium falciparum, the malaria-causing parasite, showing moderate activities. However, hybrid molecules composed of the tricyclic peroxide moiety and 7-chloro-4-aminoquinoline were synthesized and displayed a marked increase in antiplasmodial activity.

Graphical abstract: Design, synthesis and evaluation of new tricyclic endoperoxides as potential antiplasmodial agents

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Publication details

The article was received on 15 Apr 2014, accepted on 21 May 2014 and first published on 21 May 2014


Article type: Paper
DOI: 10.1039/C4OB00787E
Author version available: Download Author version (PDF)
Citation: Org. Biomol. Chem., 2014,12, 5212-5221
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    Design, synthesis and evaluation of new tricyclic endoperoxides as potential antiplasmodial agents

    J. Ruiz, S. Mallet-Ladeira, M. Maynadier, H. Vial and C. André-Barrès, Org. Biomol. Chem., 2014, 12, 5212
    DOI: 10.1039/C4OB00787E

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