Table 1.
| ||||
---|---|---|---|---|
Compds | R1 | R2 | R3 | IC50 ± SD (μM)a |
A1 | CH3 | H | 61.15 ± 3.60 | |
A2 | C2H5 | H | 33.06 ± 8.58 | |
A3 | isopropyl | H | 29.46 ± 1.64 | |
A4 | cyclohexyl | H | 9.06 ± 0.34 | |
A5 | 4-Br Phenyl | H | 6.44 ± 0.64 | |
A6 | 4-CN Phenyl | H | 19.32 ± 1.92 | |
A7 | benzyl | H | 11.39 ± 0.64 | |
A8 | CH3 | 4-CH3 | >100 | |
A9 | CH3 | 4-OCH3 | >100 | |
A10 | CH3 | 4-F | >100 | |
A11 | CH3 | 4-Cl | 85.58 ± 2.36 | |
A12 | CH3 | 4-Br | >100 | |
A13 | CH3 | 3-CH3 | 57.67 ± 2.78 | |
A14 | CH3 | 2-CH3 | 53.81 ± 8.49 | |
A15 | CH3 | H | 58.91 ± 4.58 | |
A16 | CH3 | H | 68.16 ± 2.64 | |
A17 | CH3 | H | 5.65 ± 1.40 | |
A18 | CH3 | H | 66.80 ± 2.74 | |
A19 | CH3 | H | 35.77 ± 2.96 | |
A20 | CH3 | H | 18.50 ± 0.76 | |
A21 | CH3 | H | 14.17 ± 1.30 | |
A22 | CH3 | H | 11.97 ± 0.68 | |
A23 | CH3 | H | 13.82 ± 0.90 | |
A24 | CH3 | H | >100 | |
A25 | CH3 | H | >100 | |
A26 | CH3 | H | >100 | |
A27 | CH3 | H | >100 | |
A28 | CH3 | H | >100 | |
disulfiram | – | – | – | 1.04 ± 0.03 |
The inhibitory effects of these compounds against SARS-CoV-2 3CLpro were determined by the FRET assay. The data are the mean ± SD from at least three independent experiments.