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. 2024 Apr 16;15(20):7667–7678. doi: 10.1039/d4sc01027b

Thiophene-fused γ-lactams inhibit isolated recombinant SARS-CoV-2 Mpro.

γ-Lactam aIC50 [μM]
i graphic file with name d4sc01027b-u1.jpg 8.5 ± 1.4
ii graphic file with name d4sc01027b-u2.jpg 8.4 ± 0.5
iii graphic file with name d4sc01027b-u3.jpg >100
iv graphic file with name d4sc01027b-u4.jpg >100
v graphic file with name d4sc01027b-u5.jpg >100
a

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.