S. Verbeeck, A. Yadav, B. Maes, K. Augustyns, P. Van der Veken, P. Cos, L. Maes, L. Pieters
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引用次数: 1
摘要
研究了一系列氨基取代的1-甲基-1 h - α -碳卡啉在寄生虫中的抗原性。在母体1-甲基-1 h -羰基碳环的不同位置系统地引入了不同的取代基。大多数化合物显示出有效的抗原虫活性，尽管大多数化合物对MRC-5细胞具有细胞毒性。其中一种化合物与氯喹含有相同的氨基取代，对恶性疟原虫的IC50为2.37微米，具有合理的选择性。
Antiprotozoal activity of synthetic amino substituted 1-methyl-1 H-alpha-carbolines.
The antiprotozoal properties of a series of amino substituted 1-methyl-1 H-alpha-carbolines were investigated in a broad panel of parasites. Various substituents were systematically introduced at various positions on the carbocyclic ring of the parent 1-methyl-1 H-alpha-carboline. Most compounds showed a potent antiprotozoal activity, although mostly accompanied by cytotoxicity on MRC-5 cells. One compound, containing the same amino-substitution as chloroquine, showed an IC50 against Plasmodium falciparum of 2.37 microM and was reasonably selective.
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