Table 2.
Pyridine and Pyrimidine analogs tested against TbrPDEB1
| ||||
|---|---|---|---|---|
| Compound | R1 | R2 | X | TbrPDEB1 (% inh)a |
| 11a |
|
|
C | 34.0± 22.8 |
| 11b |
|
|
C | 27.1 ± 6.1 |
| 12a |
|
|
N | 15.8 ±21.2 |
| 12b |
|
|
N | 29.8 ± 0.3 |
| 12c |
|
|
N | 12.7 ± 17.9 |
| 12d |
|
|
N | 20.6 ± 8.8 |
| 12e |
|
|
N | 32.9 ± 6.0 |
| 12f |
|
|
N | 3.9 ± 0.5 |
| 15a |
|
|
C | 48.0 ± 3.1 |
| 15b |
|
|
C | 28.4 ± 2.8 |
| 15c |
|
|
C | 7.2 ± 33 |
| 16a |
|
|
N | 14.5 ±20.5 |
| 16b |
|
|
N | 16.1 ± 22.8 |
| 16c |
|
|
N | 21.8 ± 4.6b |
| 16d |
|
|
N | 23.2 ± 10.9 |
| 16e |
|
|
N | 22.3 ± 11.2 |
| 16f |
|
|
N | 18.5 ± 5.14 |
a
Data shown are average of 2 replicate independent experiments.
b
Replicate of 4 independent experiments.