一些有机铁化合物的合成及体外杀锥虫活性评价。

Máfircio L A E Silva, Alberto F Neto, Silvia A Cardoso, Sérgio Albuquerque, Joseph Miller
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引用次数: 2

摘要

制备了八种二茂铁有机铁衍生物和二茂铁盐,并对一株克氏锥虫(Y)进行了体外抗虫试验。测定了八种有机铁化合物中的六种:二茂铁酸哌嗪1、eta(6)-(邻二甲苯)-eta(5)-(环戊二烯基)铁(II)六氟磷酸3、eta(6)-(三甲苯)-eta(5)-(环戊二烯基)铁(II)六氟磷酸5、eta(6)-(二烯二烯)-eta(5)-(环戊二烯基)铁(II)六氟磷酸6、eta(6)-(红氯甲苯)-eta(5)-(环戊二烯基)铁(II)六氟磷酸7和eta(6)-(氯苯)-eta(5)-(环戊二烯基)铁(II)苦味酸8在“体外”试验中活性较差。只有两个化合物1,1′-(n -吡啶羰基)二茂铁2(IC(50)=2.4马克/毫升)和eta(6)-(邻二甲苯)-eta(5)(环戊二烯基)铁(II)苦味酸4 (IC(50)=12.08马克/毫升)活性更高。因此,其中一些化合物有望作为预防剂用于治疗恰加斯病。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis and "in Vitro" Trypanocidal Activity Evaluation of Some Organo-iron Compounds.
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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