Table 4 Chemical structures and bioactivities of compounds 18e and 24a–d
From: An orally available Mpro/TMPRSS2 bispecific inhibitor with potent anti-coronavirus efficacy in vivo
| |||
|---|---|---|---|
Chemical modifications in R3 | |||
Compound | R3 | Mpro (nM) | TMPRSS2 (μM) |
18e |
| 233.3 ± 2.2 | 3.42 ± 0.08 |
24a |
| 159.2 ± 1.9 | 18.70 ± 3.63 |
24b |
| 155.7 ± 1.0 | 3.69 ± 0.81 |
24c |
| 69.4 ± 0.8 | 61.03 ± 3.02 |
24d (TMP1) |
| 312.5 ± 5.7 | 1.28 ± 0.43 |
