R. Di Maio et al., Synthesis and antichagasic properties of new 1,2,6-thiadiazin-3,5-dione 1,1-dioxides and related compounds, ARZNEI-FOR, 49(9), 1999, pp. 759-763
In a search for antichagasic drugs, 14 new 4-(nitroarylidene)-1,2,6-thiadia
zin-3,5-dione 1,1-dioxide derivatives were synthesized and tested in vitro
against the epimastigote form of Trypanosoma cruzi and some of them showed
important antiprotozoan activity. Attempts to synthesize new 4-(nitroarylid
ene)-3,5-diamino-1,2,6-thiadiazine 1,1-dioxides were unsuccessful. The anti
chagasic properties of nitroarylidene-malononitrile and nitroarylidene-cyan
oacetamide derivatives, thus obtained, were also tested. The cytotoxic prop
erties against Vero cells of compounds which showed remarkable in vitro ant
ichagasic activity were evaluated. All compounds tested exhibited high toxi
city percentages at 100 mu g/ml. However, compound 3c showed in vitro antic
hagasic and cytotoxic properties such as nifurtimox at the dose of 10 mu g/
ml.