Thiophene-fused γ-lactams inhibit isolated recombinant SARS-CoV-2 Mpro.
γ-Lactam | aIC50 [μM] | |
---|---|---|
i | 8.5 ± 1.4 | |
ii | 8.4 ± 0.5 | |
iii | >100 | |
iv | >100 | |
v | >100 |
Assays were performed as reported using SPE-MS, employing SARS-CoV-2 Mpro (0.05 μM) and substrate peptide (2.0 μM).42 Results are means of two independent runs each composed of technical duplicates (n = 2; mean ± standard deviation, SD). Representative dose–response curves of selected γ-lactams are shown in Fig. 2.