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. Author manuscript; available in PMC: 2011 Mar 8.
Published in final edited form as: J Med Chem. 2008 Aug 8;51(17):5176–5197. doi: 10.1021/jm800113p

Table 7.

Comparative P. falciparum and Rat PFT Inhibition Data for a Series of Inhibitors Where R = N-Boc-piperidin-4-ylmethyl

graphic file with name nihms268902t48.jpg
Compound IC50 (nM)a Selectivityb
Number X Plasmodium rat
1d graphic file with name nihms268902t49.jpg 1.2 140 117
2d graphic file with name nihms268902t50.jpg 1 ND -
3d graphic file with name nihms268902t51.jpg 1.1 150 136
6d graphic file with name nihms268902t52.jpg 350 >1000 >2.9
7d graphic file with name nihms268902t53.jpg 10 >1000 >100
9d graphic file with name nihms268902t54.jpg 3.1 ND -
a

Inhibitor concentration required to decrease P. falciparum or rat PFT activity by 50%. ND = not determined.

b

Ratio of rat to P. falciparum PFT IC50 values.