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. 2010 Nov 15;18(22):7849-54.
doi: 10.1016/j.bmc.2010.09.050. Epub 2010 Sep 25.

Synthesis and evaluation of pyrazolone compounds as SARS-coronavirus 3C-like protease inhibitors

R Ramajayam  1 , Kian-Pin Tan, Hun-Ge Liu, Po-Huang Liang
Affiliations

Synthesis and evaluation of pyrazolone compounds as SARS-coronavirus 3C-like protease inhibitors

R Ramajayam et al. Bioorg Med Chem. .

Abstract

A series of pyrazolone compounds as possible SARS-CoV 3CL protease inhibitors were designed, synthesized, and evaluated by in vitro protease assay using fluorogenic substrate peptide in which several showed potent inhibition against the 3CL protease. Interestingly, one of the inhibitors was also active against 3C protease from coxsackievirus B3. These inhibitors could be potentially developed into anti-coronaviral and anti-picornaviral agents.

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Figures

None
Graphical abstract
Figure 1
Figure 1
Pyrazole compounds as drugs or enzyme inhibitors.
Scheme 1
Scheme 1
General synthesis of compounds 2a–u.
Figure 2
Figure 2
Docking studies of 2u binding in the active site of SARS 3CLpro (A) and CVB3 3Cpro (B).
None
See this image and copyright information in PMC

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