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Issue 11, 2018
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Synthesis, characterization and biological activity of organometallic derivatives of the antimalarial drug mefloquine as new antischistosomal drug candidates

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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−1 oral dose of 3 and 4 to S. mansoni-infected mice did not significantly reduce worm burden, contrary to mefloquine.

Graphical abstract: Synthesis, characterization and biological activity of organometallic derivatives of the antimalarial drug mefloquine as new antischistosomal drug candidates

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Article information


Submitted
13 Aug 2018
Accepted
04 Oct 2018
First published
10 Oct 2018

Med. Chem. Commun., 2018,9, 1905-1909
Article type
Research Article

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, 9, 1905
DOI: 10.1039/C8MD00396C

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