Table 4.5.
Inhibition of DAT, NET, and SERT-mediated uptake of respective radioligands by thiazole-containing modafinil analogues
| Compound | Scaffold | X | Z | n | A | B | DAT (IC50 ± SD, μM) |
NET (IC50 ± SD, μM) |
SERT (IC50 ± SD, μM) |
|---|---|---|---|---|---|---|---|---|---|
| 5ll | A | H | – | – | H | H | 14.73 | 420.1 | NA |
| 5 mm | B | H | S=O | 1 | H | CH3 | 3.25 | 174 | NA |
| 5nn | B | H | S=O | 1 | H | Cyclopropyl | 4.1 ± 0.8 | 687.2 ± 152.8 | 436.1 ± 129 |
| 5oo | B | H | S=O | 1 | H | n-propyl | 28.43 ± 1.93 | NA | NA |
| 5pp | B | H | S=O | 1 | H | n-butyl | 13.50 ± 2.76 | 164 ± 56.88 | NA |
| 5qq | B | CH3 | S=O | 1 | H | H | 7.32 ± 0.04 | NA | NA |
| 5rr | B | F | S=O | 1 | H | H | 6.76 ± 0.67 | NA | NA |
| 5ss | C | CH3 | – | – | – | – | 10.57 ± 0.80 | 215.50 ± 66.01 | NA |
| 5tt | C | OCH3 | – | – | – | – | 71.59 ± 8.28 | NA | NA |
| 5uu | – | – | – | – | – | – | 0.65 ± 0.07 | 73.25 ± 9.15 | NA |