Table 2.
Biochemical activity of hybrid compounds bearing a dimethylamino-ethanol moiety as a head group and hybrid compounds bearing a naphthol moiety in core B of the biaryl scaffold
| Compound | PvNMT IC50 (nM)a | HsNMT IC50 (nM)a | SIb |
|---|---|---|---|
| 26a | 266 | >40,000 | 153.8 |
| 26b | 83.2 | 9850 | 118.4 |
| 26c | 29.4 | 4790 | 162.3 |
| 26d | 14,800 | – | – |
| 26e | 12,760 | – | – |
| 26f | 622 | >40,000 | 62.3 |
| 26g | 19,400 | – | – |
| 26h | 1563 | – | – |
| 26i | 242 | 13,860 | 57 |
| 30a | 89 | 24,010 | 269.8 |
| 30b | 19,830 | – | – |
| 30c | 248 | >40,000 | 161 |
| 30d | 7210 | – | – |
| 30e | 2880 | – | – |
| 30f | 25,400 | – | – |
aPvNMT and HsNMT IC50 values are shown as mean values of two or more determinations.
bEnzyme selectivity calculated as HsNMT IC50/PvNMT IC50.