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.