Trossini, Gustavo H. G.Malvezzi, AlbertoT-do Amaral, AntoniaRangel-Yagui, Carlota OliveiraIzidoro, Mario A.Cezari, Maria Helena S.Juliano, LuizChin, Chung Man [UNESP]Menezes, Carla M. S.Ferreira, Elizabeth Igne2014-05-202014-05-202010-02-01Journal of Enzyme Inhibition and Medicinal Chemistry. Abingdon: Taylor & Francis Ltd, v. 25, n. 1, p. 62-67, 2010.1475-6366http://hdl.handle.net/11449/7864Nitrofurazone (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 (IC(50)) for NF and NFOH presented values of 22.83 +/- 1.2 mu M and 10.55 +/- 0.81 mu M, respectively. AM1 semi-empirical molecular modeling studies were performed to understand the activity of the compounds, corroborating the observed cruzain inhibitory activity.62-67engChagas'diseasecruzain inhibitory activitymolecular modelingnitrofurazone derivativeTrypanosoma cruziArtigo10.3109/14756360902941058WOS:000275000900008Acesso restrito97343336079754130000-0003-4141-0455