4-[2-(2-Benzyloxycarbonylamino-3-t-butoxy-butyrylamino)-4-methyl-pentanoylamino]-5-(2-oxo-pyrrolidin-3-yl)-pent-2-enoic acid ethyl ester

A 3C-like protease inhibitor.

Phase of research

Potential treatment - pre-clinical evidence

How it helps

Antiviral

Drug status

Experimental

2
Supporting references
0
Contradictory references
4
AI-suggested references
0
Clinical trials

General information

4-[2-(2-Benzyloxycarbonylamino-3-t-butoxy-butyrylamino)-4-methyl-pentanoylamino]-5-(2-oxo-pyrrolidin-3-yl)-pent-2-enoic acid ethyl ester is an experimental inhibitor of SARS-CoV and SARS-CoV-2 3C-like proteases (Iketani et al., 2021; Yang et al., 2006).

4-[2-(2-Benzyloxycarbonylamino-3-t-butoxy-butyrylamino)-4-methyl-pentanoylamino]-5-(2-oxo-pyrrolidin-3-yl)-pent-2-enoic acid ethyl ester on PubChem


Synonyms

Compound 4

 

Structure image - 4-[2-(2-Benzyloxycarbonylamino-3-t-butoxy-butyrylamino)-4-methyl-pentanoylamino]-5-(2-oxo-pyrrolidin-3-yl)-pent-2-enoic acid ethyl ester

CCOC(=O)C=CC(CC1CCNC1=O)NC(=O)C(CC(C)C)NC(=O)C(C(C)OC(C)(C)C)NC(=O)OCC2=CC=CC=C2


Supporting references

Link Tested on Impact factor Notes Publication date
Lead compounds for the development of SARS-CoV-2 3CL protease inhibitors
3CLpro Crystallization Enzyme assay In vitro In silico
in silico; in vitro enzyme assay; crystallization; Vero E6 cells; SARS-CoV-2 strain 2019-nCoV/USA_WA1/2020 12.12

The compound inhibited SARS-CoV-2 3C-like protease with an IC50 of ca. 151 nM in an enzyme assay and displayed efficacy against SARS-CoV-2 infection in Vero E6 cells with an EC50 of ca. 2.9 μM.

Apr/01/2021
Inhibitors of coronavirus 3CL proteases protect cells from protease-mediated cytotoxicity
3CLpro Small molecule In vitro
HEK293T cells expressing SARS-CoV-2 3C-like protease 4.50

The compound inhibited SARS-CoV-2 3C-like protease with an EC50 of 3.023 µM in vitro.

Apr/28/2021

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