Megazol
Mostrando 1-8 de 8 artigos, teses e dissertações.
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1. In vitro genotoxicity of nitroimidazoles as a tool in the search of new trypanocidal agents
BACKGROUND Only benznidazole (Bnz) (1) and nifurtimox (Nfx) (2) are licensed for the treatment of Chagas disease although their safety and efficacy profile are far from ideal. Farmanguinhos from Fiocruz has developed seven nitroimidazole compounds (4-10) analogs of megazol (3). OBJECTIVES To evaluate whether the genotoxic effect of 3 was abolished in the
Mem. Inst. Oswaldo Cruz. Publicado em: 27/06/2019
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2. Multiple Spectroscopic and Theoretical Approaches to Study the Interaction between HSA and the Antiparasitic Drugs: Benznidazole, Metronidazole, Nifurtimox and Megazol
The interaction between four antiparasitic drugs (benznidazole (BZL), metronidazole (MTZ), nifurtimox (NFX) and megazol (MZ)) with human serum albumin (HSA), the main vehicle of biodistribution of xenobiotics, hydrophobic, small and endogenous molecules in the bloodstream, was evaluated by multiple spectroscopic techniques and theoretical calculations. In al
J. Braz. Chem. Soc.. Publicado em: 2018-07
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3. Studies of genotoxicity and mutagenicity of nitroimidazoles: demystifying this critical relationship with the nitro group
Nitroimidazoles exhibit high microbicidal activity, but mutagenic, genotoxic and cytotoxic properties have been attributed to the presence of the nitro group. However, we synthesised nitroimidazoles with activity against the trypomastigotes of Trypanosoma cruzi, but that were not genotoxic. Herein, nitroimidazoles (11-19) bearing different substituent groups
Mem. Inst. Oswaldo Cruz. Publicado em: 26/05/2015
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4. 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 compared the activity of 7 with its 4H-1,2,4-triazole bioisostere
Mem. Inst. Oswaldo Cruz. Publicado em: 18/03/2014
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5. Avaliação do potencial carcinogênico do Megazol, agente anti-chagásico, e obtenção de nanopartículas de poli(e-caprolactona) contendo Megazol. / Genotoxic evaluation of megazol, antichagasic agent and obtaining nanoparticles of poly (e-caprolactone) containing megazol.
Megazol (1-metil-2-(5-amino-1,3,4-tiadiazolil)-5-nitroimidazol) (MZ) tem sido descrito como um composto efetivo contra Tripanossoma cruzi, agente causador da Doença de Chagas. Contudo, este composto mostrou efeitos mutagênicos e baixa solubilidade em água. O primeiro objetivo desta pesquisa foi avaliar o potencial carcinogênico de três doses de MZ atrav
IBICT - Instituto Brasileiro de Informação em Ciência e Tecnologia. Publicado em: 21/10/2011
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6. Comparative study between two main obtaining routes of the Megazol / Comparação das duas principais rotas de obtenção do megazol
The scope of the present work is the analogy study over the two main routes on megazol synthesis, based on studies previously accomplished at the College of Pharmaceutical Sciences of USP. In the results of the above referred studies, it was observed that the obtaining of the megazol can be achieved by different synthetic ways, by modifying processes and rea
Publicado em: 2007
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7. SÃntese e avaliaÃÃo de atividades Anti-Toxoplama gondii e antimicrobiana de Tiossemicarbazidas, 4-Tiazolidinonas e 1,3,4-TiadiazÃis obidos a partir do Ãster 5-Metil-1H-Imidazol-4-Carboxilato de Etila
Toxoplasmosis is an infection caused by Toxoplasma gondii, a protozoan parasite with very complex biology and wide distribution in several geographical areas of the globe. In 2005, our research group published a paper reporting an exceptional anti-T. gondii activity for thiosemicarbazones and arylhydrazono-4-thiazolidinones, with a nitro group in aryl moiety
Publicado em: 2007
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8. Activity of Megazol, a Trypanocidal Nitroimidazole, Is Associated with DNA Damage
DNA damage associated with the trypanocidal activity of megazol [2-amino-5-(1-methyl-5-nitro-2-imidazolyl)-1,3,4-thiadiazole] was shown in experiments in which DNA repair-deficient RAD51−/− Trypanosoma brucei mutants were found to be hypersensitive to the drug. Parasites resistant to megazol were selected and showed modest cross-resistance to other trypa
American Society for Microbiology.