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. 2017 Oct 20;7:13683. doi: 10.1038/s41598-017-13996-8

Table 1.

Inhibitory activities of 1 and 2 on cPLA2 at 10 μM and their physiochemical properties.

graphic file with name 41598_2017_13996_Figa_HTML.gif graphic file with name 41598_2017_13996_Figb_HTML.gif
Cpd R2 m n R1 % cPLA2 Activity % Inhibition PSAa Cpd R3 q R1 % cPLA2 Activity % Inhibition PSAa
1a CF3 2 4 C5H11 40.0 ± 0.9 60.0 17.1 2a graphic file with name 41598_2017_13996_Figc_HTML.gif 2 C5H11 39.7 ± 2.6 60.3 66.4
1b CF3 2 4 C3H7 37.0 ± 3.9 63.0 17.1 2b graphic file with name 41598_2017_13996_Figd_HTML.gif 2 C5H11 26.7 ± 0.1 73.3 66.4
1c CF3 2 4 C8H17 45.0 ± 3.5 55.0 17.1 2c graphic file with name 41598_2017_13996_Fige_HTML.gif 2 C5H11 40.9 ± 1.1 59.1 66.4
1d CF3 2 4 Ph 31.8 ± 2.0 68.2 17.1 2d graphic file with name 41598_2017_13996_Figf_HTML.gif 2 C5H11 13.2 ± 1.2 86.8 66.4
1e CF3 1 4 C6H13 40.5 ± 3.6 59.5 17.1 2e graphic file with name 41598_2017_13996_Figg_HTML.gif 2 C5H11 25.8 ± 0.1 74.2 66.4
1f CF3 2 3 C5H11 33.8 ± 2.2 66.2 17.1 2f graphic file with name 41598_2017_13996_Figh_HTML.gif 2 C5H11 35.6 ± 2.1 64.4 66.4
1g CF3 2 3 C3H7 42.5 ± 0.3 57.5 17.1 2g graphic file with name 41598_2017_13996_Figi_HTML.gif 3 C5H11 15.5 ± 0.3 84.5 66.4
1h CF3 2 3 C8H17 45.6 ± 2.8 54.4 17.1 2h graphic file with name 41598_2017_13996_Figj_HTML.gif 3 C3H7 43.6 ± 0.2 56.4 66.4
1i CF3 2 2 C5H11 36.4 ± 3.3 63.6 17.1 2i graphic file with name 41598_2017_13996_Figk_HTML.gif 3 C5H11 11.5 ± 1.0 88.5 66.4
1j CF3 2 2 C7H15 33.9 ± 4.8 66.1 17.1 2j graphic file with name 41598_2017_13996_Figl_HTML.gif 3 C3H7 16.5 ± 1.2 83.5 66.4
1k CF3 2 2 C11H23 54.0 ± 6.9 46.0 17.1 2k graphic file with name 41598_2017_13996_Figm_HTML.gif 4 C5H11 37.7 ± 1.5 62.3 66.4
1l CF3 2 2 C13H27 72.4 ± 12.9 27.6 17.1 2l graphic file with name 41598_2017_13996_Fign_HTML.gif 2 C5H11 67.4 ± 5.7 32.6 72.2
1m NH2 2 4 C5H11 60.7 ± 1.9 39.3 43.1 2m graphic file with name 41598_2017_13996_Figo_HTML.gif 2 C5H11 57.5 ± 1.4 42.5 72.2
1n CClF2 2 4 C5H11 49.2 ± 4.5 50.8 17.1 2n graphic file with name 41598_2017_13996_Figp_HTML.gif 2 C5H11 33.3 ± 0.9 66.7 66.4
1o CHF2 2 4 C5H11 40.2 ± 0.5 59.8 17.1 2o graphic file with name 41598_2017_13996_Figq_HTML.gif 2 C5H11 65.5 ± 4.0 34.5 66.4
2p graphic file with name 41598_2017_13996_Figr_HTML.gif 2 C5H11 53.9 ± 2.7 46.1 89.3
2q graphic file with name 41598_2017_13996_Figs_HTML.gif 1 C5H11 56.6 ± 4.9 43.4 66.4
20c graphic file with name 41598_2017_13996_Figt_HTML.gif 2 C5H11 84.8 ± 1.0 15.2 55.4

aValues were obtained from ChemBioDraw Ultra 12.