Table 3.
Direct inhibition of bacterial ACs (ACT from B. pertussis and EF from B. anthracis) by prepared ANPpp 10a–10i and their comparison with the previously reported[17] regioisomers II (Fig. 2), where available.
| Compound | IC50
[nM][a] |
Regioisomers
IIb - IC50 [nM][a] |
||
|---|---|---|---|---|
| ACT | EF | ACT | EF | |
| 10a | 25.2 ± 5.7 | 192.7 ± 16.4 | -- | -- |
| 10b | 18.4 ± 6.6 | 174.9 ± 35.7 | -- | -- |
| 10c | 16.7 ± 0.4 | 67.3 ± 5.4 | 192 ± 13 | 235 ± 37 |
| 10d | 17.1 ± 7.1 | 263.8 ± 44 | 185 ± 31 | 428 ± 11 |
| 10e | 311.9 ± 7.3 | 7,992 ± 1,222 | -- | -- |
| 10f | 12 ± 0.2 | 120.9 ± 37.3 | 313 ± 55 | 1,335 ± 375 |
| 10g | 15.4 ± 4.5 | 5,792 ± 685 | -- | -- |
| 10h | 115.7 ± 22.4 | 162.3 ± 54.3 | 37.4 ± 7.6 | 704 ± 50 |
| 10i | 8.96 ± 0.07 | 11.6 ± 1.7 | -- | -- |
|
| ||||
| PMEApp | 17.8 ± 6.9 | 36.0 ± 2.1 | -- | -- |
[a]
Data represent the mean ± SD of at least three independent experiments.
[b]
Data taken from ref. [17].