Table 5.
In vivo anti-trypanosomal activity of 2,6-diarylpyrazine diamidine prodrugs in the GVR35 CNS mouse model.a
Codeb | Dosage (po, mg/kg)/no. of days administered | No. of mice cured c | MSDd |
---|---|---|---|
2ce(2a) | 100/5 | 3/5 | >167.8 |
3ce(3a) | 100/5 | 5/5 | >180 |
4ce(4a) | 100/5 | 5/5 | >180 |
| |||
11(10) | 100/5 | 0/5 | 69 |
12(10) | 100/5 | 2/5 | >173.8 |
100/10 | 3/4 | >180.0 | |
24b(23b) | 100/5 | 0/5 | 67.2 |
25a(23a) | 100/5 | 0/5 | 95.2 |
See Ref. 5 for details of GVR35 CNS mouse model.
Code for parent of prodrug in parenthesis.
Cure defined as survival for more than 180 days after infection without showing a parasitemia relapse.
MSD (mean survival days) was determined for mice with and without parasitemia relapse.
Data from Ref. 5