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. Author manuscript; available in PMC: 2013 Sep 13.
Published in final edited form as: J Med Chem. 2012 Aug 21;55(17):7425–7436. doi: 10.1021/jm300351w

Table 1.

Activity profiles of inhibitors 4–11a

Compd
Structure Compound code names IC50 (μM) PfDHODH EC50 (μM) Pf3D7 IC50 (μM) hDHODH IC50 (μM) PbDHODH
1* graphic file with name nihms-400824-t0001.jpg DSM1 0.047 0.076 > 100 0.23
2* graphic file with name nihms-400824-t0002.jpg DSM74 0.28 0.34 > 100 0.38
4 graphic file with name nihms-400824-t0003.jpg DSM154 > 100 >100 > 100 > 100
5 graphic file with name nihms-400824-t0004.jpg DSM155 > 100 > 50 > 100 > 100
6 graphic file with name nihms-400824-t0005.jpg DSM71 0.15±0.01 0.19 (0.15 – 0.25) > 100 2.8±0.28
7 graphic file with name nihms-400824-t0006.jpg DSM96 4.8±0.7 5.2 (3.6 – 6.7) n.d. 6.3±0.80
8 graphic file with name nihms-400824-t0007.jpg DSM68 0.4±0.09 0.91 (0.80 – 1.0) > 100 3.3±0.4
9 graphic file with name nihms-400824-t0008.jpg DSM23 0.44±0.17 2.2 (1.2 – 3.7) > 100 11±3.3
10 graphic file with name nihms-400824-t0009.jpg DSM70 > 100 > 12.5 n.d. n.d.
11 graphic file with name nihms-400824-t0010.jpg DSM105 > 50 > 5 n.d. >50
12 graphic file with name nihms-400824-t0011.jpg DSM25 4.8±0.38 3.2 (2.4 – 3.5) n.d. > 10
13 graphic file with name nihms-400824-t0012.jpg DSM78 27±6.3 > 10 n.d. n.d.
14 graphic file with name nihms-400824-t0013.jpg DSM79 >25 3.2 (2.4 – 4.3) n.d. n.d.
15 graphic file with name nihms-400824-t0014.jpg DSM80 > 100 > 25 n.d. n.d.
16 graphic file with name nihms-400824-t0015.jpg DSM151 0.077 ± 0.008 0.32 (0.30 – 0.35) > 100 0.17 ± 0.018
*

Data for DSM1 and DSM74 were taken from27,29 For enzyme data the error represents the standard error of the fit for n=3 data points per concentration; for parasite data the error displayed is the 95% confidence interval of the fit for n=3 or 4 data points per concentration.