Departamento de Química, Universidade Estadual de Maringá, Avenida Colombo, 5790, Zona 7, 87020-900, Maringá, PR, Brazil.
Biomed Pharmacother. 2010 Jul;64(6):386-9. doi: 10.1016/j.biopha.2010.02.006. Epub 2010 Mar 10.
A series of 1-phenylsubstituted beta-carbolines containing an N-butylcarboxamide group at C-3 of beta-carboline nucleus were synthesized and evaluated in vitro against epimastigote form of Trypanosoma cruzi and promastigote form of Leishmania amazonensis. Among all compounds tested, two derivatives (2b and 2d) presented potent activity against both parasites. The most active derivative 2b showed also the higher selectivity index ratio (SI) for L. amazonensis (SI=2,084). The effect of other N-alkylcarboxamide groups at C-3, such as pyrrolidyl, N-cyclohexil and N-benzylcarboxamide on T. cruzi and L. amazonensis activity was also evaluated. Our results pointed the synthesized beta-carboline-3-carboxamide derivatives as potential compounds for new drugs for Chagas' disease and leishmaniasis' treatment.
合成了一系列 1-苯取代的β-咔啉类化合物，其中β-咔啉核的 C-3 位上含有 N-丁基羧酰胺基团，并对其进行了体外抗锥虫属克鲁兹体（Trypanosoma cruzi）的前鞭毛体和利什曼原虫属亚马逊利什曼原虫（Leishmania amazonensis）的前鞭毛体的活性评价。在所测试的所有化合物中，有两个衍生物（2b 和 2d）对两种寄生虫均具有很强的活性。最具活性的衍生物 2b 对利什曼原虫属亚马逊利什曼原虫的选择性指数比（SI）也最高（SI=2.084）。还评估了其他 N-烷基羧酰胺基团，如吡咯烷基、N-环己基和 N-苄基羧酰胺在 T. cruzi 和 L. amazonensis 活性方面的影响。我们的研究结果表明，所合成的β-咔啉-3-羧酰胺衍生物具有作为治疗恰加斯病和利什曼病新药的潜力。
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