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. Author manuscript; available in PMC: 2014 Nov 1.
Published in final edited form as: Bioorg Med Chem. 2013 Aug 13;21(21):10.1016/j.bmc.2013.08.006. doi: 10.1016/j.bmc.2013.08.006

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
a

See Ref. 5 for details of GVR35 CNS mouse model.

b

Code for parent of prodrug in parenthesis.

c

Cure defined as survival for more than 180 days after infection without showing a parasitemia relapse.

d

MSD (mean survival days) was determined for mice with and without parasitemia relapse.

e

Data from Ref. 5