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. 2019 Nov 25;7:798. doi: 10.3389/fchem.2019.00798

Table 2.

Cruzain inhibition and trypanocidal activity of compounds with modifications to the hydrophobic fragment and the amide function.

graphic file with name fchem-07-00798-i0022.jpg
Compound Structure IC50 cruzain (μM)a IC50 T. cruzi (μM)b
10h graphic file with name fchem-07-00798-i0023.jpg 1.4 ± 0.8 >100
10j graphic file with name fchem-07-00798-i0024.jpg 0.6 ± 0.1 1.0 ± 0.3
7 graphic file with name fchem-07-00798-i0025.jpg ND 1.5 ± 0.4
a

IC50 values against cruzain were independently determined by obtaining rate measurements in triplicate for at least six inhibitor concentrations. The values represent the mean ± SD of three individual experiments.

b

IC50 values against T. cruzi represent the mean ± SD of two individual experiments. ND, not determined.