Potent inhibitors of SARS-CoV-2 3C-like protease derived from N-substituted isatin compounds

SARS-CoV-2 3C-like protease is the main protease of SARS-CoV-2 and has been considered as one of the key targets for drug discovery against COVID-19. We identified several N-substituted isatin compounds as potent SARS-CoV-2 3C-like protease inhibitors. The three most potent compounds inhibit SARS-Co...

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Autores principales: Liu, Pei, Liu, Hongbo, Sun, Qi, Liang, Hao, Li, Chunmei, Deng, Xiaobing, Liu, Ying, Lai, Luhua
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Masson SAS. 2020
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7395831/
https://www.ncbi.nlm.nih.gov/pubmed/32798789
http://dx.doi.org/10.1016/j.ejmech.2020.112702
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author Liu, Pei
Liu, Hongbo
Sun, Qi
Liang, Hao
Li, Chunmei
Deng, Xiaobing
Liu, Ying
Lai, Luhua
author_facet Liu, Pei
Liu, Hongbo
Sun, Qi
Liang, Hao
Li, Chunmei
Deng, Xiaobing
Liu, Ying
Lai, Luhua
author_sort Liu, Pei
collection PubMed
description SARS-CoV-2 3C-like protease is the main protease of SARS-CoV-2 and has been considered as one of the key targets for drug discovery against COVID-19. We identified several N-substituted isatin compounds as potent SARS-CoV-2 3C-like protease inhibitors. The three most potent compounds inhibit SARS-CoV-2 3C-like protease with IC(50)’s of 45 nM, 47 nM and 53 nM, respectively. Our study indicates that N-substituted isatin compounds have the potential to be developed as broad-spectrum anti-coronavirus drugs.
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spelling pubmed-73958312020-08-03 Potent inhibitors of SARS-CoV-2 3C-like protease derived from N-substituted isatin compounds Liu, Pei Liu, Hongbo Sun, Qi Liang, Hao Li, Chunmei Deng, Xiaobing Liu, Ying Lai, Luhua Eur J Med Chem Article SARS-CoV-2 3C-like protease is the main protease of SARS-CoV-2 and has been considered as one of the key targets for drug discovery against COVID-19. We identified several N-substituted isatin compounds as potent SARS-CoV-2 3C-like protease inhibitors. The three most potent compounds inhibit SARS-CoV-2 3C-like protease with IC(50)’s of 45 nM, 47 nM and 53 nM, respectively. Our study indicates that N-substituted isatin compounds have the potential to be developed as broad-spectrum anti-coronavirus drugs. Elsevier Masson SAS. 2020-11-15 2020-08-01 /pmc/articles/PMC7395831/ /pubmed/32798789 http://dx.doi.org/10.1016/j.ejmech.2020.112702 Text en © 2020 Elsevier Masson SAS. 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
Liu, Pei
Liu, Hongbo
Sun, Qi
Liang, Hao
Li, Chunmei
Deng, Xiaobing
Liu, Ying
Lai, Luhua
Potent inhibitors of SARS-CoV-2 3C-like protease derived from N-substituted isatin compounds
title Potent inhibitors of SARS-CoV-2 3C-like protease derived from N-substituted isatin compounds
title_full Potent inhibitors of SARS-CoV-2 3C-like protease derived from N-substituted isatin compounds
title_fullStr Potent inhibitors of SARS-CoV-2 3C-like protease derived from N-substituted isatin compounds
title_full_unstemmed Potent inhibitors of SARS-CoV-2 3C-like protease derived from N-substituted isatin compounds
title_short Potent inhibitors of SARS-CoV-2 3C-like protease derived from N-substituted isatin compounds
title_sort potent inhibitors of sars-cov-2 3c-like protease derived from n-substituted isatin compounds
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7395831/
https://www.ncbi.nlm.nih.gov/pubmed/32798789
http://dx.doi.org/10.1016/j.ejmech.2020.112702
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