Table 2. Binding Affinity of Methylated Compounds Determined by [3H]PiB Competition Assays on αSYN fibrils.
| # | R | n | N-substitution | Ki (nM) |
|---|---|---|---|---|
| RB1 | H | 1 | N-piperidine | >400 |
| RB2 | H | 1 | N-(N-methyl)piperazine | >400 |
| 1b | 4-CH3 | 1 | N-piperidine | 36.1; 83.9 |
| 2b | 4-OCH3 | 1 | N-piperidine | 70.8; 34.3 |
| 3b | 4-F | 1 | N-piperidine | >400 |
| 4b | 5-CH3 | 1 | N-piperidine | 84.6; 59.9 |
| 5b | 5-OCH3 | 1 | N-piperidine | 27.5; 162.9 |
| 6b | 5-F | 1 | N-piperidine | 435.2; 268.2 |
| 7b | 6-CH3 | 1 | N-piperidine | 16.8; 23.8 |
| 8b | 6-OCH3 | 1 | N-piperidine | 19.7; 9.6 |
| 9b | 6-F | 1 | N-piperidine | 335.4; 43.6 |
| 10b | 7-CH3 | 1 | N-piperidine | 231.3; 63.9 |
| 11b | 7-OCH3 | 1 | N-piperidine | 233.7; 177.3 |
| 12b | 7-F | 1 | N-piperidine | >400 |
| 13b | H | 0 | N-piperidine | >400 |
| 14b | H | 2 | N-piperidine | 23.0; 16.8 |
| 15b | H | 1 | N-morpholine | >400 |
| 16b | H | 1 | N-thiomorpholine | >400 |
| 17b | H | 1 | N-pyrrolidine | 144.7; 58.6 |
| 18b | H | 1 | N-fluoropiperidine | >400 |
| 19b | H | 1 | N-dimethylamine | >400 |