Synthesis, characterization and biological activity of organometallic derivatives of the antimalarial drug mefloquine as new antischistosomal drug candidates
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Faustine d'Orchymont Jeannine Hess Gordana Panic Marta Jakubaszek Lea Gemperle Jennifer Keiser Gilles GasserAbstract
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.
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Journal MedChemComm
Volume 9
Issue number 11
Pages 1905-1909
Available online
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Publisher website (DOI) 10.1039/c8md00396c
Europe PubMed Central 30568758
Pubmed 30568758
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