Synthesis and potent antiprotozoal activity of mono/di amidino 2-anilinobenzimidazoles versus Plasmodium falciparum and Trypanosoma brucei rhodesiense
Synthesis and potent antiprotozoal activity of mono/di amidino 2-anilinobenzimidazoles versus Plasmodium falciparum and Trypanosoma brucei rhodesiense
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DOI：
10.1016/j.bmc.2016.06.047
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发表时间：
2016-09-15
影响因子：
3.5
通讯作者：
Goker, Hakan
中科院分区：
文献类型：
--
作者：
Karaaslan, Cigdem;Kaiser, Marcel;Goker, Hakan
以4-氨基-3-硝基苯甲腈和相应的邻苯二胺为原料，经四步反应合成了一系列单阳离子的新型2-苯胺基苯并咪唑甲胺。体外测定了它们对恶性疟原虫和罗德氏锥虫的抗寄生活性。与氯喹相比，部分阳离子化合物(10，12，14)与美拉索前列醇具有相同或非常接近的抗恶性疟原虫活性，也显示出与氯喹相同或非常接近的抗恶性疟原虫活性。在单阳离子衍生物中，化合物21对恶性疟原虫的抑制活性最强。(C)2016爱思唯尔有限公司。保留所有权利。
A series of mono and dicationic new 2-anilinobenzimidazole carboxamidines were prepared in a four step process starting from 4-amino-3-nitrobenzonitrile and corresponding o-phenylenediamines. Their antiparasitic activity against Plasmodium falciparum (P. falciparum) and Trypanosoma brucei rhodesiense (T. b. rhodesiense) were evaluated in vitro. Some of the dicationic compounds (10,12,14) showed equal or very close activity against T. b. rhodesiense with melarsoprol and also showed promising activity against P. falciparum as compared to chloroquine. Among the monocationic derivatives compound 21 exhibited best inhibitory activity against P. falciparum. (C) 2016 Elsevier Ltd. All rights reserved.