Table 1.
Effect of the substitution of the aromatic ring Aa
 | ||||
|---|---|---|---|---|
| Compound | Method and Yield (%) | R2 | IC50 ± SD (µM) ROCK1 | IC50 ± SD (µM) ROCK2 |
| 5a | b, 35%; h, 69% |  |
0.17 ± 0.01 (6) | 0.05 ± 0 (6) |
| 5b | e, 63% |  |
0.027 ± 0.005 (8) | 0.011 ± 0.002 (6) |
| 5c | b, 31% |  |
1.40 ± 0.11 (6) | 0.47 ± 0.03 (6) |
| 5d | j, 74% |  |
ROCK1% inhibition @ 50 µM: 9.1 ± 1.6 | ND |
| 5e | e, 35% |  |
0.05 ± 0.009 (12) | 0.02 ± 0.008 (12) |
| 5f | e, 82% |  |
37.8 ± 7.8 (6) | 31.1 ± 9.1 (6) |
| 5g | g, 59% |  |
0.008 ± 0.001 (10) | 0.006 ± 0.001 (9) |
| 5h | e, 77% |  |
0.62 ± 0.019 (6) | 0.28 ± 0.05 (6) |
| 5i | e, 74% |  |
0.38 ± 0.046 (6) | 0.14 ± 0.029 (6) |
| 5j | i, 90% |  |
1.2 ± 0.4 (3) | 0.18 ± 0.04 (3) |
| 5k | e, 44% |  |
0.56 ± 0.10 (3) | 0.10 ± 0.03 (3) |
| 5l | e, 22% |  |
1.3 ± 0.2 (3) | 0.13 ± 0.02 (3) |
| 5m | e, 50% |  |
0.50 ± 0.05 (6) | 0.24 ± 0.03 (6) |
| 5n | e, 87% |  |
2.1 ± 0.6 (3) | 0.29 ± 0.17 (3) |
| 5o | e, 80% |  |
3.36 ± 1.00 (3) | 0.68 ± 0.43 (3) |
| 5p | e, 84% |  |
13.0 ± 1.4 (3) | 3.44 ± 0.87 (3) |
| 5q | b, 5%; e, 73% |  |
0.10 ± 0.02 (6) | 0.05 ± 0.01 (6) |
| 5r | b, 64% |  |
0.40 ± 0.03 (6) | 0.12 ± 0.01 (6) |
| 5s | b, 16% |  |
0.57 ± 0.05 (6) | 0.19 ± 0.00 (6) |
| 5t | e, 54% |  |
0.14 ± 0.02 (6) | 0.06 ± 0.01 (6) |
| 5u | b, 12% |  |
0.34 ± 0.02 (6) | 0.11 ± 0.01 (6) |
| 5v | e, 86% |  |
2.4 ± 0.5 (6) | 1.1 ± 0.2 (6) |
| 5w | e, 59% |  |
0.46 ± 0.08 (6) | 0.12 ± 0.03 (6) |
| 5x | e, 48% |  |
0.15 ± 0.03 (6) | 0.12 ± 0.02 (6) |
| 5y | e, 77% |  |
5.2 ± 0.5 (6) | 2.0 ± 0.15 (6) |
a
Key: number of repeats shown in parentheses.