Table 1.
Mac1 Inhibition data for secondary amino acid derivatives. IC50s, changes in the melting temperature and corresponding SDs of three replicates are given.
| Compound | Structure | R group | Stereochem | SARS CoV2 Mac1 Alpha (µM) | Δ Tm (°C) @300 µM |
|---|---|---|---|---|---|
| 5a |  |
Me | (S) | 130 ± 5.7 | |
| 6a | H | (S) | 241 ± 5.2 | ||
| 5b |  |
Me | NA | >300 | |
| 6b | H | NA | 111 ± 4.2 | ||
| 6c |  |
H | (S) | 227 ± 6.1 | |
| 5d | Me | (R) | >300 | ||
| 6d | H | (R) | 246 ± 14.3 | ||
| 6e |  |
H | (S) | 57.8 ± 2.8 | |
| 5f | Me | (R) | 150 ± 1.6 | ||
| 6f | H | (R) | 64.7 ± 3.7 | ||
| 5g |  |
Et | racemic | 127 ± 12.9 | |
| 6g | H | racemic | 21.6 ± 2.1 | 1.67 ± 0.01 | |
| 10a |  |
Me | (S) | Inactive | |
| 12a | H | (S) | 68.6 ± 2.6 | ||
| 10b | Me | (R) | Inactive | ||
| 12b | H | (R) | 266.7 ± 14.7 | ||
| 5h |  |
Et | NA | 63.8 ± 8.9 | |
| 6h | H | NA | 23.5 ± 1.5 | 1.24 ± 0.21 |