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. Author manuscript; available in PMC: 2009 Dec 25.
Published in final edited form as: J Med Chem. 2008 Dec 25;51(24):8027–8037. doi: 10.1021/jm800649q

Table 1. Inhibition of PLA2 by fluoroketones.

Average percent inhibition and standard error (n=3) reported for each compound at 0.091 mole fraction. XI(50) values determined for inhibitors with greater than 90% inhibition. N.D. signifies compounds with less than 25% inhibition (or no detectable inhibition).

No Structure GIVA cPLA2 GVIA iPLA2 GV sPLA2
% Inhibition XI(50) % Inhibition XI(50) % Inhibition XI(50)
6 graphic file with name nihms86631t1.jpg 96 ± 2 0.0223 ± 0.0023 92 ± 3 0.0195 ± 0.0053 79 ± 9
11 graphic file with name nihms86631t2.jpg N.D. 50 ± 13 43 ± 8
8 graphic file with name nihms86631t3.jpg 38 ± 2 96 ± 3 0.0096 ±0.0008 N.D.
10a graphic file with name nihms86631t4.jpg N.D. 98 ± 16 0.0073 ± 0.0007 28 ± 1
12a graphic file with name nihms86631t5.jpg 62 ± 5 96 ± 6 0.0025 ± 0.0003 48 ± 6
10b graphic file with name nihms86631t6.jpg 56 ± 4 98 ± 5 0.0065 ± 0.001 46 ± 8
12b graphic file with name nihms86631t7.jpg 68 ± 6 99 ± 10 0.0018 ± 0.0005 53 ± 14
10c graphic file with name nihms86631t8.jpg 65 ± 12 98 ± 4 0.0065 ± 0.0008 75 ± 10
19a graphic file with name nihms86631t9.jpg 91 ± 2 0.0199 ± 0.0025 85 ± 4 0.0328 ±0.0035 82 ± 8
20a graphic file with name nihms86631t10.jpg 92 ± 3 0.0098 ± 0.0006 91 ± 4 0.0169 ±0.0021 86 ± 2
19b graphic file with name nihms86631t11.jpg 96 ± 2 0.0156 ± 0.0019 94 ± 8 0.0208 ±0.0032 80 ± 6
20b graphic file with name nihms86631t12.jpg 95 ± 2 0.0116 ± 94 ± 8 94 ± 8 0.0166 ±0.0022 84 ± 7
23 graphic file with name nihms86631t13.jpg 88 ± 1 71 ± 14 49 ± 12
21 graphic file with name nihms86631t14.jpg 73 ± 4 95 ± 5 0.0075 ±0.0011 86 ± 4
30 graphic file with name nihms86631t15.jpg 27 ± 3 49 ± 12 59 ± 12
26 graphic file with name nihms86631t16.jpg 94 ± 2 0.0167 ± 0.0018 93 ± 4 0.0011 ± 0.0002 86 ± 10 0.0236 ± 0.004
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