Departamento de Parasitologia, Microbiologia e Imunologia, ICB, Universidade Federal de Juiz de Fora, Campus Universitário, Rua José Lourenço Kelmer, 36036-900 Juiz de Fora, Minas Gerais, Brazil.
Biomed Pharmacother. 2011 Jul;65(4):313-6. doi: 10.1016/j.biopha.2011.03.003. Epub 2011 May 30.
The high incidence of malaria and drug-resistant strains of Plasmodium have turned this disease into a problem of major health importance. One of the approaches used to control it is to search for new antimalarial agents, such as quinoline derivates. This class of compounds composes a broad group of antimalarial agents, which are largely employed, and inhibits the formation of β-haematin (malaria pigment), which is lethal to the parasite. More specifically, 4-aminoquinoline derivates represent potential sources of antimalarials, as the example of chloroquine, the most used antimalarial worldwide. In order to assess antimalarial activity, 12 4-aminoquinoline derived drugs were obtained and some of these derivatives were used to obtain platinum complexes platinum (II). These compounds were tested in vivo in a murine model and revealed remarkable inhibition of parasite multiplication values, whose majority ranged from 50 to 80%. In addition they were not cytotoxic. Thus, they may be object of further research for new antimalarial agents.
疟疾的高发病率和抗药性疟原虫菌株已使这种疾病成为一个重大的健康问题。控制疟疾的方法之一是寻找新的抗疟药物，如喹啉衍生物。这类化合物组成了一大类抗疟药物，广泛应用于抑制β-血红素（疟色素）的形成，这对寄生虫是致命的。更具体地说，4-氨基喹啉衍生物是抗疟药物的潜在来源，例如氯喹，它是世界上使用最广泛的抗疟药物。为了评估抗疟活性，获得了 12 种 4-氨基喹啉衍生药物，其中一些衍生物被用于获得铂(II)配合物。这些化合物在体内进行了小鼠模型试验，结果显示对寄生虫增殖的抑制作用显著，大多数抑制率在 50%至 80%之间。此外，它们没有细胞毒性。因此，它们可能成为进一步研究新型抗疟药物的对象。
