New thiadiazine derivatives with activity against Trypanosoma cruzi amastigotes
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 cyt...
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Published in | Folia parasitologica Vol. 48; no. 2; pp. 105 - 108 |
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Main Authors | , , , , , , |
Format | Journal Article |
Language | English |
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Czech Republic
01.01.2001
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Abstract | 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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AbstractList | 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. |
Author | Di Maio, R Cerecetto, H Muelas, S Seoane, G Gómez-Barrio, A Escario, J A Ochoa, C |
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BackLink | https://www.ncbi.nlm.nih.gov/pubmed/11437122$$D View this record in MEDLINE/PubMed |
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SubjectTerms | Animals Antiprotozoal Agents - pharmacology Chagas Disease - drug therapy Macrophages - drug effects Macrophages - parasitology Mice Parasitic Sensitivity Tests Thiadiazines - pharmacology Trypanosoma cruzi - drug effects |
Title | New thiadiazine derivatives with activity against Trypanosoma cruzi amastigotes |
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