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

Table 1.

Cruzain inhibition and trypanocidal activity of compounds with modifications to the imide nucleus.

graphic file with name fchem-07-00798-i0001.jpg
Compound Structure IC50 cruzain (μM)a IC50 T. cruzi (μM)b
Initial hit (3a) graphic file with name fchem-07-00798-i0002.jpg 2.2 ± 0.4 >100
10b graphic file with name fchem-07-00798-i0003.jpg 4.2 ± 1.5 >100
10c graphic file with name fchem-07-00798-i0004.jpg 2.3 ± 1.0 0.9 ± 0.3
10d graphic file with name fchem-07-00798-i0005.jpg 12.0 ± 1.0 18.5 ± 3.1
10e graphic file with name fchem-07-00798-i0006.jpg 2.5 ± 0.6 1.2 ± 0.3
10f graphic file with name fchem-07-00798-i0007.jpg 0.6 ± 0.1 2.0 ± 0.7
10k graphic file with name fchem-07-00798-i0008.jpg ND >100
10l graphic file with name fchem-07-00798-i0009.jpg ND 11.6 ± 2.4
10m graphic file with name fchem-07-00798-i0010.jpg ND 1.8 ± 0.4
10n graphic file with name fchem-07-00798-i0011.jpg ND 1.6 ± 0.5
10o graphic file with name fchem-07-00798-i0012.jpg ND 1.7 ± 0.5
BZ - ND 3.0 ± 0.6
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.