| Author | Castro, Solange L. de | |
| Author | Meirelles, Maria de Nazareth L. de | |
| Access date | 2020-09-14T18:45:07Z | |
| Available date | 2020-09-14T18:45:07Z | |
| Document date | 1990 | |
| Citation | CASTRO, Solange L. de; MEIRELLES, Maria de Nazareth L. Mechanism of action of a nitroimidazole-thiadiazole derivate upon Trypanosoma cruzi tissue culture amastigotes. Memórias do Instituto Oswaldo Cruz, Rio de Janeiro, v. 85, n. 1, p. 95-99, jan./mar. 1990. | pt_BR |
| ISSN | 0074-0276 | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/43360 | |
| Language | eng | pt_BR |
| Publisher | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. | pt_BR |
| Rights | open access | |
| Subject in Portuguese | Trypanosoma cruzi | pt_BR |
| Subject in Portuguese | Agentes quimioterápicos | pt_BR |
| Subject in Portuguese | Amastigotas | pt_BR |
| Subject in Portuguese | Biossíntese de macromoléculas | pt_BR |
| Subject in Portuguese | Precursores radioativos | pt_BR |
| Subject in Portuguese | Ação do derivado de tiadiazol | pt_BR |
| Subject in Portuguese | Megazol | pt_BR |
| Title | Mechanism of action of a Nitroimidazole-Thiadiazole derivate upon Trypanosoma cruzi tissue culture amastigotes | pt_BR |
| Type | Article | |
| DOI | 10.1590/S0074-02761990000100016 | |
| Abstract | Megazol (CL 64,855) a very effective drug in experimental infections by Trypanosoma cruzi, and also in in vitro assays with vertebrate forms of the parasite, had its parasite, had its activity upon macromolecule biosynthesis tested using tissue culture-derived amastigote forms. Megazol presented a drastic inhibition of [3H]-uridine incorporation, suggesting a selective activity upon protein synthesis. Comparing the three drugs, megazol was more potent than nifurtimox and benznidazole in inhibiting protein an DNA synthesis. Megazol showed a 91% of inhibition of [3H]-leucine incorporation whereas nifurtimox and benznidazole, 0% and 2%, respectively. These latter two drugs inhibited the incorporation of all the precursors tested at similar levels, but the concentration of benznidazole was always three times higher, suggesting different mechanisms of action or, more probably, a greater efficiency of the 5-nitrofuran derivate in relation to the 2-nitroimidazole. So, wes conclude that the mode of action of megazol is different from the ones of nifurtimox and benznidazole and that its primary effect is associated with an impairment of protein synthesis. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Ultraestrutura e Biologia Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Ultraestrutura e Biologia Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Subject | Trypanosoma cruzi | pt_BR |
| Subject | Chemoterapeutic agents | pt_BR |
| Subject | Amastigotes | pt_BR |
| Subject | Macromolecule biosynthesis | pt_BR |
| Subject | Radiactive precursors | pt_BR |
| Subject | Action of thiadiazole derivate | pt_BR |
| Subject | Megazol | pt_BR |
| e-ISSN | 1678-8060 | |
