Table 1.
Structures and activity of 3-chloropyridinyl ester-derived SARS-CoV-2 3CLpro inhibitors.
Entry | Entry Compound Structure | SARS CoV-2 3CLpro IC50 (μM) | SARS-CoV-2 EC50 (μM)a |
---|---|---|---|
| |||
1 |
![]() |
0.25 | 2.8 |
2 |
![]() |
0.32 | 15 |
3 |
![]() |
0.31 | 43.7 |
4 |
![]() |
0.12 | 69.8 |
5 |
![]() |
0.90 | 8.1 |
6 |
![]() |
0.073 | 15 |
7 |
![]() |
0.38 | 11.5 |
8 |
![]() |
0.47 | 56.7 |
9 |
![]() |
10.3 | >100 |
10 |
![]() |
0.59 | 3.1 |
11 |
![]() |
0.87 | 14 |
12 |
![]() |
0.34 | >100 |
13 |
![]() |
0.49 | 57.1 |
14 |
![]() |
1.19 | >100 |
15 |
![]() |
0.42 | >100 |
Compounds 3 and 4 exhibited antiviral EC50 values 3.4 μM and 3.2 μM, respectively.