Table 3.
Scaffold | Entry | Comp | Scaffold | R2 | 1% O2 IC50 (uM) |
---|---|---|---|---|---|
1 | 20 | A | 4-F | inactive | |
2 | 21 | A | 2-tBu | inactive | |
3 | 22 | A | 2-NO2 | inactive | |
4 | 1 | A | 2-EtO | 0.43 | |
5 | 23 | A | H | inactive | |
6 | 24 | A | 2-Cl | inactive | |
7 | 25 | A | 2-Me | inactive | |
8 | 26 | A | 2-Benzyloxy | inactive | |
9 | 27 | A | 2-F | inactive | |
10 | 28 | A | 2-PhO | inactive | |
11 | 29 | A | 2-MeO | 3.3 | |
12 | 30 | A | 2-CF3 | inactive | |
13 | 31 | B | 2-MeO, 5-CF3 | 0.2 | |
14 | 32 | B | 2-MeO, 5-NO2 | 4.2 | |
15 | 42 | B | 2-EtNH | 4.1 | |
16 | 33 | B | 2-Benzyloxy | 22.9 | |
17 | 34 | B | 2-isobutoxy | 6.2 | |
18 | 35 | B | 2-EtS | 3.5 | |
19 | 36 | B | 4-MeO | inactive | |
20 | 16 | B | 2-EtO | 0.09 |
Values of IC50 are the mean of three independent experiments.