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. 2013 Dec 4;56(24):10158–10170. doi: 10.1021/jm401610c

Table 3. Preliminary PK/PD Assessment for Compounds Dosed Orally at 20 mg/kg for up to 10 Days to Mice Infected with T. cruzia.

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compd IC50 (μM) plasma concn, 0.5 h (μM) plasma concn, 24 h (μM) parasites cleared from blood during 10-day dosing?
47 0.024 3.31 0.016 no
48 0.013 1.29 0.008 no
49 0.061 3.26 0.001 no
4 0.019 2.42 0.002 no
50 0.047 5.29 0.002 no
51 0.058 3.28 0.001 no
5 0.011 0.85 0.490 yes
2 0.012 2.49 0.030 yes
52 0.002 1.37 0.047 yes
6 0.017 5.54 0.790 yes
(rac)-7 0.007 1.55 0.370 yes
posaconazole 0.001 3.04 2.89 yes
a

Plasma exposure data were obtained in a parallel group of noninfected mice following a single oral dose of 20 mg/kg.