. Author manuscript; available in PMC: 2023 Sep 19.

Published in final edited form as: J Med Chem. 2021 Sep 16;64(19):14702–14714. doi: 10.1021/acs.jmedchem.1c01214

Table 2.

Structures and activity of substituted active ester-derived SARS-CoV-2 3CLpro inhibitors.

Entry	SARS-CoV-2 3CLpro IC₅₀(μM)	SARS-CoV-2 EC₅₀ (μM)^a

1	100	>100
2	100	>100
3	>100	>100
4	2.2	19.3
5	15.3	30
6	4.4	57

Compounds 3 and 4 exhibited antiviral EC₅₀ values 3.4 μM and 3.2 μM, respectively.