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Issue 11, 2012
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Synthesis of precursors and macrocycle analogs of aerucyclamides as anti-trypanosomal agents

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Abstract

In the search for candidates of antiparasitic new drugs, macrocycle analogs and key fragments of aerucyclamides were obtained. The activities against Trypanosoma brucei brucei and cytotoxicities on murine macrophages (cell line J774) were evaluated. Two of the prepared compounds displayed similar anti-trypanosomal activities as aerucyclamides B and C. In addition, the compound with the highest activity presents a 150-fold selectivity (SI = 150) for the parasite than against the murine macrophage.

Graphical abstract: Synthesis of precursors and macrocycle analogs of aerucyclamides as anti-trypanosomal agents

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Publication details

The article was received on 27 Jul 2012, accepted on 06 Sep 2012 and first published on 10 Sep 2012


Article type: Concise Article
DOI: 10.1039/C2MD20218B
Med. Chem. Commun., 2012,3, 1443-1448

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    Synthesis of precursors and macrocycle analogs of aerucyclamides as anti-trypanosomal agents

    S. Peña, L. Scarone, A. Medeiros, E. Manta, M. Comini and G. Serra, Med. Chem. Commun., 2012, 3, 1443
    DOI: 10.1039/C2MD20218B

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