Laboratório de Química Sintética e Heterocíclica, Instituto de Ciências Exatas, Departamento de Química, Av. Antônio Carlos, 6627 Pampulha, UFMG, 31270-901 Belo Horizonte, MG, Brazil.
Eur J Med Chem. 2012 Jun;52:304-12. doi: 10.1016/j.ejmech.2012.03.039. Epub 2012 Mar 29.
Five 2-hydroxy-3-substituted-aminomethyl naphthoquinones, nine 1,2,3-triazolic para-naphthoquinones, five nor-β-lapachone-based 1,2,3-triazoles, and several other naphthoquinonoid compounds were synthesized and evaluated against the infective bloodstream form of Trypanosoma cruzi, the etiological agent of Chagas disease, continuing our screening program for new trypanocidal compounds. Among all the substances, 16-18, 23, 25-29 and 30-33 were herein described for the first time and fifteen substances were identified as more potent than the standard drug benznidazole, with IC(50)/24h values in the range of 10.9-101.5 μM. Compounds 14 and 19 with Selectivity Index of 18.9 and 6.1 are important structures for further studies.
合成了 5 种 2-羟基-3-取代氨甲基萘醌、9 种 1,2,3-三唑对萘醌、5 种诺-β-拉帕醌基 1,2,3-三唑和其他几种萘醌类化合物，并对恰加斯病的病原体克氏锥虫的感染性血红细胞形式进行了评估，这是我们筛选新型杀锥虫化合物的计划的延续。在所有这些物质中，16-18、23、25-29 和 30-33 是首次被描述的，其中 15 种物质的活性强于标准药物苯并咪唑，其 IC(50)/24h 值在 10.9-101.5 μM 范围内。化合物 14 和 19 的选择性指数分别为 18.9 和 6.1，这是进一步研究的重要结构。
