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

Org Biomol Chem

Laboratoire de Synthèse et de Physicochimie de Molécules d'Intérêt Biologique, UMR CNRS 5068, Université Paul-Sabatier, 118 route de Narbonne, F-31062 Toulouse cedex 4, France.

Published: July 2014

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.

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Source
http://dx.doi.org/10.1039/c4ob00787eDOI Listing

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