Folia Parasitologica 48[2] 105-108 (2001) | DOI: 10.14411/fp.2001.015

New thiadiazine derivatives with activity against Trypanosoma cruzi amastigotes

Susana Muelas¹, Rossanna Di Maio², Hugo Cerecetto², Gustavo Seoane², Carmen Ochoa³, José Antonio Escario¹, Alicia Gómez-Barrio¹

¹ Departamento de Parasitología, Facultad de Farmacia, Universidad Complutense, Ciudad Universitaria s/n, 28040 Madrid, Spain

² Departamento de Química Orgánica, Facultad de Químicas, Universidad de la República, cc 1157, 11800-Montevideo, Uruguay

³ Instituto de Química Médica, Consejo Superior de Investigaciones Científicas, C/ Juan de la Cierva 3, 28003 Madrid, Spain

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 µg/ml. Only one of the compounds had an anti-amastigote activity similar to that of reference drugs at 10 µg/ml, but unfortunately this disappeared at lower concentrations.

Keywords: anti-Trypanosoma cruzi drugs, amastigotes, J774 macrophages, cytotoxicity assay

Received: June 19, 2000; Accepted: September 12, 2000; Published: June 1, 2001  Show citation