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Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors
N-Substituted isatin derivatives were prepared from the reaction of isatin and various bromides via two steps. Bioactivity assay results (in vitro tests) demonstrated that some of these compounds are potent and selective inhibitors against SARS coronavirus 3CL protease with IC(50) values ranging fro...
| Autores principales: | , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
Elsevier Ltd.
2005
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| Materias: | |
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7119080/ https://www.ncbi.nlm.nih.gov/pubmed/15896959 http://dx.doi.org/10.1016/j.bmcl.2005.04.027 |
| _version_ | 1783514702132805632 |
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| author | Chen, Li-Rung Wang, Yu-Chin Lin, Yi Wen Chou, Shan-Yen Chen, Shyh-Fong Liu, Lee Tai Wu, Ying-Ta Kuo, Chih-Jung Chen, Tom Shieh-Shung Juang, Shin-Hun |
| author_facet | Chen, Li-Rung Wang, Yu-Chin Lin, Yi Wen Chou, Shan-Yen Chen, Shyh-Fong Liu, Lee Tai Wu, Ying-Ta Kuo, Chih-Jung Chen, Tom Shieh-Shung Juang, Shin-Hun |
| author_sort | Chen, Li-Rung |
| collection | PubMed |
| description | N-Substituted isatin derivatives were prepared from the reaction of isatin and various bromides via two steps. Bioactivity assay results (in vitro tests) demonstrated that some of these compounds are potent and selective inhibitors against SARS coronavirus 3CL protease with IC(50) values ranging from 0.95 to 17.50 μM. Additionally, isatin 4o exhibited more potent inhibition for SARS coronavirus protease than for other proteases including papain, chymotrypsin, and trypsin. |
| format | Online Article Text |
| id | pubmed-7119080 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2005 |
| publisher | Elsevier Ltd. |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-71190802020-04-03 Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors Chen, Li-Rung Wang, Yu-Chin Lin, Yi Wen Chou, Shan-Yen Chen, Shyh-Fong Liu, Lee Tai Wu, Ying-Ta Kuo, Chih-Jung Chen, Tom Shieh-Shung Juang, Shin-Hun Bioorg Med Chem Lett Article N-Substituted isatin derivatives were prepared from the reaction of isatin and various bromides via two steps. Bioactivity assay results (in vitro tests) demonstrated that some of these compounds are potent and selective inhibitors against SARS coronavirus 3CL protease with IC(50) values ranging from 0.95 to 17.50 μM. Additionally, isatin 4o exhibited more potent inhibition for SARS coronavirus protease than for other proteases including papain, chymotrypsin, and trypsin. Elsevier Ltd. 2005-06-15 2005-05-17 /pmc/articles/PMC7119080/ /pubmed/15896959 http://dx.doi.org/10.1016/j.bmcl.2005.04.027 Text en Copyright © 2005 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 Chen, Li-Rung Wang, Yu-Chin Lin, Yi Wen Chou, Shan-Yen Chen, Shyh-Fong Liu, Lee Tai Wu, Ying-Ta Kuo, Chih-Jung Chen, Tom Shieh-Shung Juang, Shin-Hun Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors |
| title | Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors |
| title_full | Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors |
| title_fullStr | Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors |
| title_full_unstemmed | Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors |
| title_short | Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors |
| title_sort | synthesis and evaluation of isatin derivatives as effective sars coronavirus 3cl protease inhibitors |
| topic | Article |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7119080/ https://www.ncbi.nlm.nih.gov/pubmed/15896959 http://dx.doi.org/10.1016/j.bmcl.2005.04.027 |
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