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

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 act...

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Autores principales: Ramajayam, R., Tan, Kian-Pin, Liu, Hun-Ge, Liang, Po-Huang
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Ltd. 2010
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7127448/
https://www.ncbi.nlm.nih.gov/pubmed/20947359
http://dx.doi.org/10.1016/j.bmc.2010.09.050
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author Ramajayam, R.
Tan, Kian-Pin
Liu, Hun-Ge
Liang, Po-Huang
author_facet Ramajayam, R.
Tan, Kian-Pin
Liu, Hun-Ge
Liang, Po-Huang
author_sort Ramajayam, R.
collection PubMed
description 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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spelling pubmed-71274482020-04-08 Synthesis and evaluation of pyrazolone compounds as SARS-coronavirus 3C-like protease inhibitors Ramajayam, R. Tan, Kian-Pin Liu, Hun-Ge Liang, Po-Huang Bioorg Med Chem Article 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. Elsevier Ltd. 2010-11-15 2010-09-25 /pmc/articles/PMC7127448/ /pubmed/20947359 http://dx.doi.org/10.1016/j.bmc.2010.09.050 Text en Copyright © 2010 Elsevier Ltd. All rights reserved. Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.
spellingShingle Article
Ramajayam, R.
Tan, Kian-Pin
Liu, Hun-Ge
Liang, Po-Huang
Synthesis and evaluation of pyrazolone compounds as SARS-coronavirus 3C-like protease inhibitors
title Synthesis and evaluation of pyrazolone compounds as SARS-coronavirus 3C-like protease inhibitors
title_full Synthesis and evaluation of pyrazolone compounds as SARS-coronavirus 3C-like protease inhibitors
title_fullStr Synthesis and evaluation of pyrazolone compounds as SARS-coronavirus 3C-like protease inhibitors
title_full_unstemmed Synthesis and evaluation of pyrazolone compounds as SARS-coronavirus 3C-like protease inhibitors
title_short Synthesis and evaluation of pyrazolone compounds as SARS-coronavirus 3C-like protease inhibitors
title_sort synthesis and evaluation of pyrazolone compounds as sars-coronavirus 3c-like protease inhibitors
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7127448/
https://www.ncbi.nlm.nih.gov/pubmed/20947359
http://dx.doi.org/10.1016/j.bmc.2010.09.050
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