Design, synthesis, and antimalarial activity of structural chimeras of thiosemicarbazone and ferroquine analogues
Design, synthesis, and antimalarial activity of structural chimeras of thiosemicarbazone and ferroquine analogues
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DOI：
10.1016/j.bmcl.2007.10.003
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发表时间：
2007-12-01
影响因子：
2.7
通讯作者：
Chibale, Kelly
中科院分区：
文献类型：
--
作者：
Biot, Christophe;Pradines, Bruno;Chibale, Kelly
本文报道了硫代氨基脲（TSC）与亚铁喹（FQ）嵌合体的设计、合成及其抗疟活性。从FQ衍生出的关键结构元素被耦合到能够配位金属离子的碎片上。对4株恶性疟原虫和寄生半胱氨酸蛋白酶falcipin -2进行了生物学评价。为了确定二茂铁基部分在该系列抗疟原虫活性中的作用，还合成并测试了纯有机母体化合物。氨基喹啉结构的存在，使化合物能够运输到寄生虫的食物液泡中，似乎是抗疟疾活性的主要贡献者。(c) 2007 Elsevier Ltd.版权所有。
The design, synthesis, and antimalarial activity of chimeras of thiosemicarbazones (TSC) and ferroquine (FQ) is reported. Key structural elements derived from FQ were coupled to fragments capable of coordinating metal ions. Biological evaluation was conducted against four strains of the malaria parasite Plasmodium falciparum and against the parasitic cysteine protease falcipain-2. To establish the role of the ferrocenyl moiety in the antiplasmodial activity of this series, purely organic parent compounds were also synthesized and tested. The presence of the aminoquinoline structure, allowing transport of the compounds to the food vacuole of the parasite, seems to be the major contributor to antimalarial activity. (c) 2007 Elsevier Ltd. All rights reserved.