羟甲基硝呋酮和硝呋酮对克氏锥虫的抑制作用：对一种新的靶标的研究。
Cruzain inhibition by hydroxymethylnitrofurazone and nitrofurazone: investigation of a new target in Trypanosoma cruzi.
机构信息
Departamento de Farmácia, Faculdade de Ciências Farmacêuticas, USP, São Paulo, Brazil.
出版信息
J Enzyme Inhib Med Chem. 2010 Feb;25(1):62-7. doi: 10.3109/14756360902941058.
Nitrofurazone (NF) and its derivative, hydroxymethylnitrofurazone (NFOH), have presented antichagasic activity. NFOH has higher activity and lower mutagenicity. The aim of this work was to assess whether NF and its derivative NFOH would also be inhibitors of cruzain, besides their trypanothione reductase inhibitory activity. In vitro cruzain inhibition tests were performed for both compounds, and the 50% inhibitory concentration (IC50) for NF and NFOH presented values of 22.83 +/- 1.2 microM and 10.55 +/- 0.81 microM, respectively. AM1 semi-empirical molecular modeling studies were performed to understand the activity of the compounds, corroborating the observed cruzain inhibitory activity.
硝呋太尔（NF）及其衍生物羟甲基硝呋太尔（NFOH）具有抗查加斯病活性。NFOH 具有更高的活性和更低的致突变性。本工作旨在评估 NF 及其衍生物 NFOH 是否也会抑制克氏锥虫 cruzain，除了它们的 trypanothione 还原酶抑制活性。对两种化合物进行了体外 cruzain 抑制试验，NF 和 NFOH 的 50%抑制浓度（IC50）分别为 22.83 +/- 1.2 microM 和 10.55 +/- 0.81 microM。进行了 AM1 半经验分子建模研究，以了解化合物的活性，证实了观察到的 cruzain 抑制活性。
Zotero 插件