Table 2. a Analogs exploring the Region A of 3.
| Compound | R1 | TbrPDEB1 (% inh) |
TbrPDEB1 (IC50 μM) |
TbrPDEB2 (IC50 μM) |
|---|---|---|---|---|
| 17a |
|
94 ± 3.5 | 6.4 ± 1.7 | 6.2 ± 0.6 |
| 17b |
|
37 ± 14 | ||
| 17c |
|
6 ±1.4 | - | |
| 17d |
|
54 ± 8.8 | - | |
| 17e |
|
50 ± 6.1 | - | |
| 17f |
|
35 ± 10 | 23 ± 4.0 | |
| 17g |
|
65 ± 5.5 | ndb | |
| 17h |
|
9 ±7.1 | - | |
| 17i |
|
8.6 ± 5.2 | - | |
| 17j |
|
74 ± 13 | 9 ± 0.6 | |
| 17k |
|
10 ± 6.9 | - | |
| 17l |
|
43 ±16 | - | |
| 17m |
|
83± 7.5 | 6.7 ± 2.9 | 4.6± 0.1 |
| 17n |
|
13 ± 8 | - | |
| 17o |
|
83 ± 1.3 | 6 ± 1.7 | |
| 17p |
|
53 ± 24 | 5.9 ± 0.4 | |
| 17q |
|
27 ± 8.3 | - | |
| 17r |
|
31 ± 6.3 | - | |
| 17s |
|
68 ± 6.3 | 12 ± 2.7 | |
| 17t |
|
85 ± 6.5 | 5.9 ±1.0 | 13.5 ± 3.5 |
| 17u |
|
52 ± 8.3 | - | |
| 17v |
|
43 ± 3.3 | - | |
| 18a |
|
10 ± 5.3 | - | |
| 18b |
|
31 ±14 | - | |
| 19a |
|
84 ± 9.1 | 3.1 ± 0.5 | 8.0 ± 3.9 |
a
All values are the mean of three or more replicates ± SEM.
b
No IC50 obtained due to limited solubility at higher concentrations.