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. Author manuscript; available in PMC: 2017 Oct 1.
Published in final edited form as: Bioorg Med Chem. 2016 Jul 27;24(19):4544–4554. doi: 10.1016/j.bmc.2016.07.057

Table 1.

Inhibition of PLA2 by 2-oxoamidesa

Number Structure ClogPb GIVA cPLA2 GVIA iPLA2 GV sPLA2
% Inhibition XI(50) % Inhibition XI(50) % Inhibition
AX04828 graphic file with name nihms809927t1.jpg 7.61 0.022 ± 0.009 0.027 ± 0.009
AX00628 graphic file with name nihms809927t2.jpg 6.63 0.024 ± 0.015 N.D.
25b graphic file with name nihms809927t3.jpg 7.39 49.3 ±2.0 94.7 ±0.5 0.014± 0.003 40.6 ±5.9
25a graphic file with name nihms809927t4.jpg 6.30 >85 0.020 ± 0.006 95.1 ±0.6 0.013 ± 0.003 33.8 ±6.0
27b graphic file with name nihms809927t5.jpg 6.41 >85 0.023 ± 0.005 N.D. N.D.
27a graphic file with name nihms809927t6.jpg 5.32 >85 0.016 ± 0.004 N.D. N.D.
32 graphic file with name nihms809927t7.jpg 4.94 63.6 ±2.6 81.1 ±1.0 N.D.
27d graphic file with name nihms809927t8.jpg 4.82 88.0 ±0.9 0.013 ± 0.002 82.5 ±1.4 N.D.
25c graphic file with name nihms809927t9.jpg 5.69 59.3 ±3.1 N.D. N.D.
27c graphic file with name nihms809927t10.jpg 4.71 N.D. N.D. N.D.
28 graphic file with name nihms809927t11.jpg 4.61 N.D. N.D. N.D.
a

Average percent inhibition and standard error (n = 3) are reported for each compound at 0.091 mol fraction. XI(50) values were determined for inhibitors with greater than 85% inhibition. N.D. signifies compounds with less than 25% inhibition (or no detectable inhibition).

b

Calculated by ChemOffice Ultra 11.00.