Table 1.
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 | 2 | C5H11 | 39.7 ± 2.6 | 60.3 | 66.4 | |
1b | CF3 | 2 | 4 | C3H7 | 37.0 ± 3.9 | 63.0 | 17.1 | 2b | 2 | C5H11 | 26.7 ± 0.1 | 73.3 | 66.4 | |
1c | CF3 | 2 | 4 | C8H17 | 45.0 ± 3.5 | 55.0 | 17.1 | 2c | 2 | C5H11 | 40.9 ± 1.1 | 59.1 | 66.4 | |
1d | CF3 | 2 | 4 | Ph | 31.8 ± 2.0 | 68.2 | 17.1 | 2d | 2 | C5H11 | 13.2 ± 1.2 | 86.8 | 66.4 | |
1e | CF3 | 1 | 4 | C6H13 | 40.5 ± 3.6 | 59.5 | 17.1 | 2e | 2 | C5H11 | 25.8 ± 0.1 | 74.2 | 66.4 | |
1f | CF3 | 2 | 3 | C5H11 | 33.8 ± 2.2 | 66.2 | 17.1 | 2f | 2 | C5H11 | 35.6 ± 2.1 | 64.4 | 66.4 | |
1g | CF3 | 2 | 3 | C3H7 | 42.5 ± 0.3 | 57.5 | 17.1 | 2g | 3 | C5H11 | 15.5 ± 0.3 | 84.5 | 66.4 | |
1h | CF3 | 2 | 3 | C8H17 | 45.6 ± 2.8 | 54.4 | 17.1 | 2h | 3 | C3H7 | 43.6 ± 0.2 | 56.4 | 66.4 | |
1i | CF3 | 2 | 2 | C5H11 | 36.4 ± 3.3 | 63.6 | 17.1 | 2i | 3 | C5H11 | 11.5 ± 1.0 | 88.5 | 66.4 | |
1j | CF3 | 2 | 2 | C7H15 | 33.9 ± 4.8 | 66.1 | 17.1 | 2j | 3 | C3H7 | 16.5 ± 1.2 | 83.5 | 66.4 | |
1k | CF3 | 2 | 2 | C11H23 | 54.0 ± 6.9 | 46.0 | 17.1 | 2k | 4 | C5H11 | 37.7 ± 1.5 | 62.3 | 66.4 | |
1l | CF3 | 2 | 2 | C13H27 | 72.4 ± 12.9 | 27.6 | 17.1 | 2l | 2 | C5H11 | 67.4 ± 5.7 | 32.6 | 72.2 | |
1m | NH2 | 2 | 4 | C5H11 | 60.7 ± 1.9 | 39.3 | 43.1 | 2m | 2 | C5H11 | 57.5 ± 1.4 | 42.5 | 72.2 | |
1n | CClF2 | 2 | 4 | C5H11 | 49.2 ± 4.5 | 50.8 | 17.1 | 2n | 2 | C5H11 | 33.3 ± 0.9 | 66.7 | 66.4 | |
1o | CHF2 | 2 | 4 | C5H11 | 40.2 ± 0.5 | 59.8 | 17.1 | 2o | 2 | C5H11 | 65.5 ± 4.0 | 34.5 | 66.4 | |
2p | 2 | C5H11 | 53.9 ± 2.7 | 46.1 | 89.3 | |||||||||
2q | 1 | C5H11 | 56.6 ± 4.9 | 43.4 | 66.4 | |||||||||
20c | 2 | C5H11 | 84.8 ± 1.0 | 15.2 | 55.4 |
aValues were obtained from ChemBioDraw Ultra 12.