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Developing selective cruzain inhibitors through structure-based techniques
(Universidade Federal de Minas GeraisBrasilICB - DEPARTAMENTO DE BIOQUÍMICA E IMUNOLOGIAPrograma de Pós-Graduação em Bioquímica e ImunologiaUFMG, 2017-02-16)
Cruzain is the major Trypanosoma cruzi cysteine proteinase, a validated target for drug development against this parasite. T. cruzi is the etiological agent of Chagas Disease, a pathological condition from Latin America, ...
Biochemical evaluation of a series of synthetic chalcone and hydrazide derivatives as novel inhibitors of cruzain from Trypanosoma cruzi
(Sociedade Brasileira de Química - SBQSão Paulo, 2010)
Chagas’ disease, a parasitic infection widely distributed throughout Latin America, is a major public health problem with devastating consequences in terms of human morbidity and mortality. The enzyme cruzain is the major ...
Convergent synthesis and cruzain inhibitory activity of novel 2-(N `-benzylidenehydrazino)-4-trifluoromethyl-pyrimidines
(PERGAMON-ELSEVIER SCIENCE LTD, 2008)
To search for new cruzain inhibitors, the synthesis of a series of novel 2-(N`-benzylidenehydrazino)-4-trifluoromethyl-pyrimidines in a convergent manner is presented. The cruzain inhibitory activity of some of these ...
Cruzain inhibition by hydroxymethylnitrofurazone and nitrofurazone: investigation of a new target in Trypanosoma cruzi
(TAYLOR & FRANCIS LTD, 2010)
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 ...
Cruzain inhibition by hydroxymethylnitrofurazone and nitrofurazone: investigation of a new target in Trypanosoma cruzi
(Taylor & Francis Ltd, 2010-02-01)
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 ...
Inhibition of cysteine proteases by a natural biflavone: behavioral evaluation of fukugetin as papain and cruzain inhibitor
(Informa HealthcareLondon, 2013-08)
Cruzain is the major cysteine protease of Trypanosoma cruzi, the infectious agent responsible for Chagas disease, and cruzain inhibitors display considerable antitrypanosomal activity. In the present work we elucidated ...
Identification and characterization of cruzain allosteric inhibitors: a computer-aided approach
(Universidade Estadual Paulista (Unesp), 2017-09-29)
Trypanosoma cruzi é o agente causal da doença de Chagas, uma infecção negligenciada que afeta milhões de pessoas nas regiões tropicais. A maioria dos fármacos empregados no tratamento desta doença são altamente tóxicos e ...
Síntese, ensaios in vitro e estudos computacionais de aminoquinolinas possíveis inibidoras da cruzaína e rodesaína
(Universidade Federal de Minas GeraisUFMG, 2016-02-24)
In this work a series of aminoquinolines, potential inhibitors of cruzain and rhodesain, was synthesized, evaluated on in vitro assays and studied by in silico methods. Chagas disease is caused by Tripanossoma cruzi and ...