Table 3.
Compound | R1 substituent | βH inhibition IC50 (μM) |
---|---|---|
15a | Nitro | 4.3 ± 0.1 |
15b | 4.7 ± 0.7 | |
15c | 7.0 ± 0.2 | |
| ||
15d | Cyano | 6.34 ± 0.09 |
15e | 4.4 ± 0.2 | |
| ||
15f | Methyl | 8 ± 1 |
15g | >1000 | |
| ||
15h | tert-Butyl | 13.3 ± 0.7 |
15i | 6.8 ± 0.1 | |
15j | >1000 | |
| ||
15k | H | 507 ± 33 |
15l | >1000 | |
| ||
15m | Methoxy | 22 ± 1 |
15n | > 1000 | |
| ||
15o | H (X = N) | 260 ± 7 |
15p | >1000 | |
| ||
20 | N/A | 21 ± 1 |
| ||
CQ | N/A | 31.5 ± 0.5 |