Acute toxicity of novel N-sulfonylpyrimidine derivatives in vivo

The aim of the present study was to investigate in vivo toxic effects and to find acute toxic doses (LD50) of novel N-sulfonyl derivatives of pyrimidine nucleobases uracil and cytosine. Six N-1-sulfonyluracil derivatives (1, 2, 6, 7, 8, and 9) and two N-1-sulfonylcytosine (4, 12) and N-1,NH-4-disulfonylcytosine (13) were evaluated in this study. All experiments were performed on 10-14week-old male and female c57bl/6 zgr mice weighing 22-25 g at the time of treatment. The obtained data showed that derivatives 1, 2, 7, 12 and 13 cause less toxicity than derivatives 4, 6, 8 and 9. Compounds 2, 7, 12 and 13 did not cause death in mice in doses of 3000 mg/kg. Uracil derivative 8 has shown the highest toxicity, its acute toxic dose being 150 mg/kg, similar to the acute toxic dose of 5-fluorouracil.