New thiadiazine derivatives with activity against Trypanosoma cruzi amastigotes
Language English Country Czech Republic Media print
Document type Journal Article
PubMed
11437122
DOI
10.14411/fp.2001.015
Knihovny.cz E-resources
- MeSH
- Antiprotozoal Agents pharmacology MeSH
- Chagas Disease drug therapy MeSH
- Macrophages drug effects parasitology MeSH
- Mice MeSH
- Parasitic Sensitivity Tests MeSH
- Thiadiazines pharmacology MeSH
- Trypanosoma cruzi drug effects MeSH
- Animals MeSH
- Check Tag
- Mice MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Names of Substances
- Antiprotozoal Agents MeSH
- Thiadiazines MeSH
The cytotoxicity of 18 new 1,2,6-thiadiazin-3,5-dione 1,1-dioxides was evaluated. This group of products was previously assayed against epimastigotes of Trypanosoma cruzi and some of them showed a high antiprotozoal activity. Thereafter 13 compounds with a high anti-epimastigote activity and low cytotoxicity were selected to be assayed against amastigotes. Some of the products showed the same or even lower cytotoxicity than nifurtimox and benznidazole, but most of them were very toxic for macrophages at 100 microg/ml. Only one of the compounds had an anti-amastigote activity similar to that of reference drugs at 10 microg/ml, but unfortunately this disappeared at lower concentrations.
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