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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 2.

In vitro and in vivo anti-trypanosomal activity of 2,6-diarylpyrazine diamidines in the STIB900 mouse model.a

Code T. b. r.
IC50(nM)
Dosage (ip, mg/kg) b Cures c Survival (days) d
1 2.2 20 2/4 >57.5
5 1/4 >38
2a 4.5 20 3/4 >57.75
5 1/4 >46
3a 6.5 20 4/4 >60
5 3/4 >54.5
4a 21 20 4/4 >60
5 3/4 >49.5
6 18 5 0/4 36.5
10 5.8 5 3/4 >53.5
15a 462 / / /
15b 27 5 0/4 >41
19a 14 5 4/4 >60
19b 6 5 2/4 >60
23a 37 5 2/4 >53.75
23b 4.8 5 1/4 >36.5
a

See Refs. 5 and 18 for details of STIB900 mouse model.

b

Daily dosage was administered for 4 days; ip, intraperitoneal.

c

Number of mice that survive and are parasite free for 60 days.

d

Average days of survival; untreated control expires between day 7 and 9 post-infection.