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Synthesis, Characterization and Biological Activity of Organometallic Derivatives of the Antimalarial Drug Mefloquine as New Antischistosomal Drug Candidates

Abstract

We present the design, synthesis, characterization and biological evaluation of new ferrocenyl and ruthenocenyl derivatives of the organic antimalarial mefloquine, a drug also known for its antischistosomal activity. The two metallocenyl derivatives prepared (3 and 4) demonstrated comparable activity to mefloquine against adult-stage Schistosoma mansoni in vitro. Importantly, both compounds were found to have lower toxicity in all cell lines than mefloquine itself. Administration of a 200 mg/kg oral dose of 3 and 4 to S. mansoni-infected mice did not significantly reduce worm burden, contrary to mefloquine.

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Publication details

The article was received on 13 Aug 2018, accepted on 04 Oct 2018 and first published on 10 Oct 2018


Article type: Research Article
DOI: 10.1039/C8MD00396C
Citation: Med. Chem. Commun., 2018, Accepted Manuscript
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    Synthesis, Characterization and Biological Activity of Organometallic Derivatives of the Antimalarial Drug Mefloquine as New Antischistosomal Drug Candidates

    F. D'Orchymont, J. Hess, G. Panic, M. Jakubaszek, L. Gemperle, J. Keiser and G. Gasser, Med. Chem. Commun., 2018, Accepted Manuscript , DOI: 10.1039/C8MD00396C

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