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Int J Med Chem. 2015;2015:458319. doi: 10.1155/2015/458319. Epub 2015 Feb 05.

Design and Synthesis of Novel Hybrid Molecules against Malaria.

International journal of medicinal chemistry

Melanie Lödige, Luisa Hiersch

Affiliations

  1. Institute of Organic Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany.

PMID: 25734014 PMCID: PMC4334980 DOI: 10.1155/2015/458319

Abstract

The effective treatment of malaria can be very complex: Plasmodium parasites develop in multiple stages within a complex life cycle between mosquitoes as vectors and vertebrates as hosts. For the full and effective elimination of parasites, an effective drug should be active against the earliest stages of the Plasmodium infection: liver stages (reduce the progress of the infection), blood stages (cure the clinical symptoms), and gametocytes (inhibit the transmission cycle). Towards this goal, here we report the design, the synthetic methodology, and the characterization of novel hybrid agents with combined activity against Plasmodium liver stages and blood stages and gametocytes. The divergent synthetic approach allows the access to differently linked primaquine-chloroquine hybrid templates in up to eight steps.

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