硫代氨基脲、氨基酰基硫代氨基脲和酰基噻唑烷酮对克氏锥虫的合成、对接及体外活性
Synthesis, docking, and in vitro activity of thiosemicarbazones, aminoacyl-thiosemicarbazides and acyl-thiazolidones against Trypanosoma cruzi.
作者信息
Leite Ana Cristina Lima, de Lima Renata Souza, Moreira Diogo Rodrigo de M, Cardoso Marcos Veríssimo de O, Gouveia de Brito Ana Carolina, Farias Dos Santos Luciene Maria, Hernandes Marcelo Zaldini, Kiperstok Alice Costa, de Lima Ricardo Santana, Soares Milena B P
机构信息
Avaliação e Síntese de Fármacos-LABSINFA, Departamento de Ciências Farmacêuticas, Universidade Federal de Pernambuco, Rua Prof. Artur Sá S/N, Cidade Universitária, 50740-520 Recife, PE, Brazil.
出版信息
Bioorg Med Chem. 2006 Jun 1;14(11):3749-57. doi: 10.1016/j.bmc.2006.01.034. Epub 2006 Feb 3.
A novel series of thiosemicarbazone and aminoacyl-thiazolidones derivatives were synthesized. Their structure suggests that these compounds could have anti-Trypanosoma cruzi activity. Biological evaluation indicates that some of these compounds are able to inhibit the growth of T. cruzi in concentrations non-cytotoxic to mammalian cells. Docking studies were carried out in order to investigate the binding pattern of these compounds for the T. cruzi cruzain (TCC) protein, and these showed a significant correlation with experimental data.
合成了一系列新型的硫代半卡巴腙和氨酰基噻唑烷酮衍生物。它们的结构表明这些化合物可能具有抗克氏锥虫活性。生物学评估表明，其中一些化合物能够在对哺乳动物细胞无细胞毒性的浓度下抑制克氏锥虫的生长。进行了对接研究以探究这些化合物与克氏锥虫克鲁兹蛋白酶（TCC）的结合模式，结果显示与实验数据有显著相关性。
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