Table 1. Mean inhibition percentages of the 19 coumarin-based derivatives (1a–p and 2a–c) against SARS-CoV-2 Mpro at 100 µM using the FRET assay.
| ||
|---|---|---|
| Compound | R | Mean inhibition% |
| 1a | 4-Cl-3-CF3 | 3.0 |
| 1b | 3,5-(CF3)2 | 7.4 |
| 1c | 3-Cl-4-F | 36.7 |
| 1d | 3-CF3 | 31.9 |
| 1e | 4-CF3 | 65.9 |
| 1f | 3,5-Di-Cl | 56.7 |
| 1g | 2,4-Di-Cl | 12.0 |
| 1h | 4-F | 32.8 |
| 1i | 4-Br | 7.7 |
| 1j | 4-n-Butyl | 15.6 |
| 1k | 3,5-Di-CH3 | 33.5 |
| 1l | 4-Butoxy | 31.6 |
| 1m | 4-Cl-2-CH3 | 0.1 |
| 1n | 2-Cl-6-CH3 | 4.8 |
| 1o | 2,4-Di-F | 14.5 |
| 1p | 2,6-Di-Br-4-F | 18.2 |
| 2a | 4-Cl-3-CF3 | 22.2 |
| 2b | 3,5-(CF3)2 | 0.9 |
| 2c | 2,4-Di-F | 0.7 |
| GC376 | — | 100.0 |
| Boceprevir | — | 88.0 |
| Baicalein | — | 100.1 |