Synthesis and “in Vitro” Trypanocidal Activity Evaluation of Some Organo-iron Compounds.

Abstract

Eight organo-iron ferrocene derivatives and arenocenium salts were prepared and evaluated by “in vitro” assay against one strain of Trypanosoma cruzi (Y). Six of the eight organo-iron compounds assayed, piperazinium diferrocenoate 1, η⁶-(o-xylene)-η⁵-(cyclopentadienyl) Iron(II) hexafluorophosphate 3, η⁶-(mesitylene)-η⁵-(cyclopentadienyl) iron(II) hexafluorphosphate 5, η⁶-(durene)-η⁵-(cyclopentadienyl) iron(II) hexafluorphosphate 6, η⁶-(ρ-chlorotoluene)-η⁵-(cyclopentadienyl) Iron(II) hexafluorphosphate 7 and η⁶-(chlorobenzene)-η⁵-(cyclopentadienyl) iron(II) picrate 8 , were poorly active in the “in vitro” assays. Only two compounds 1,1'–(N-pyperidinocarbonyl) ferrocene 2(IC₅₀=2.4 μg/mL) and η⁶-(o-xylene)-η⁵(cyclopentadienyl) iron(II) picrate 4 (IC₅₀=12.08 μg/mL), were more active. Thus, some of the compounds are promising to be used against Chagas' disease as a prophylactic agents.

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