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Megazol and its bioisostere 4H-1,2,4-triazole: comparing the trypanocidal, cytotoxic and genotoxic activities and their in vitro and in silico interactions with the Trypanosoma brucei nitroreductase enzyme

Megazol (7) is a 5-nitroimidazole that is highly active against Trypanosoma cruzi and Trypanosoma brucei, as well as drug-resistant forms of trypanosomiasis. Compound 7 is not used clinically due to its mutagenic and genotoxic properties, but has been largely used as a lead compound. Here, we compar...

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Main Authors: Alcione Silva de Carvalho, Kelly Salomão, Solange Lisboa de Castro, Taline Ramos Conde, Helena Pereira da Silva Zamith, Ernesto Raúl Caffarena, Belinda Suzette Hall, Shane Robert Wilkinson, Núbia Boechat
Format: Artigo
Language:Inglês
Published: Fundação Oswaldo Cruz (FIOCRUZ) 2014-06-01
Series:Memorias do Instituto Oswaldo Cruz
Subjects:
megazol
Trypanosoma cruzi
Trypanosoma brucei
T. brucei
nitroreductase
genotoxicity
Online Access:http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762014000300315&lng=en&tlng=en
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