Synthesis, characterization and biological activity of organometallic derivatives of the antimalarial drug mefloquine as new antischistosomal drug candidatesElectronic supplementary information (ESI) available. See DOI: 10.1039/c8md00396c

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. The design, synthesis, characterization and biological evaluation of new ferrocenyl and ruthenocenyl derivatives of the antimalarial mefloquine is described.