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New quinoline-triazole conjugates: Synthesis, and antiviral properties against SARS-CoV-2
At present therapeutic options for severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) are very limited. We designed and synthesized three sets of small molecules using quinoline scaffolds. A series of quinoline conjugates (10a-l, 11a-c, and 12a-e) by incorporating 1,2,3-triazole were synth...
Autores principales: | , , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier Inc.
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8219945/ https://www.ncbi.nlm.nih.gov/pubmed/34214752 http://dx.doi.org/10.1016/j.bioorg.2021.105117 |
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author | Seliem, Israa A. Panda, Siva S. Girgis, Adel S. Moatasim, Yassmin Kandeil, Ahmed Mostafa, Ahmed Ali, Mohamed A. Nossier, Eman S. Rasslan, Fatma Srour, Aladdin M. Sakhuja, Rajeev Ibrahim, Tarek S. Abdel-samii, Zakaria K.M. Al-Mahmoudy, Amany M.M. |
author_facet | Seliem, Israa A. Panda, Siva S. Girgis, Adel S. Moatasim, Yassmin Kandeil, Ahmed Mostafa, Ahmed Ali, Mohamed A. Nossier, Eman S. Rasslan, Fatma Srour, Aladdin M. Sakhuja, Rajeev Ibrahim, Tarek S. Abdel-samii, Zakaria K.M. Al-Mahmoudy, Amany M.M. |
author_sort | Seliem, Israa A. |
collection | PubMed |
description | At present therapeutic options for severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) are very limited. We designed and synthesized three sets of small molecules using quinoline scaffolds. A series of quinoline conjugates (10a-l, 11a-c, and 12a-e) by incorporating 1,2,3-triazole were synthesized via a modified microwave-assisted click chemistry technique. Among the synthesized conjugates, 4-((1-(2-chlorophenyl)-1H-1,2,3-triazol-4-yl)methoxy)-6-fluoro-2-(trifluoromethyl)quinoline (10g) and 6-fluoro-4-(2-(1-(4-methoxyphenyl)-1H-1,2,3-triazol-4-yl)ethoxy)-2-(trifluoromethyl)quinoline (12c) show high potency against SARS-CoV-2. The selectivity index (SI) of compounds 10g and 12c also indicates the significant efficacy compared to the reference drugs. |
format | Online Article Text |
id | pubmed-8219945 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | Elsevier Inc. |
record_format | MEDLINE/PubMed |
spelling | pubmed-82199452021-06-23 New quinoline-triazole conjugates: Synthesis, and antiviral properties against SARS-CoV-2 Seliem, Israa A. Panda, Siva S. Girgis, Adel S. Moatasim, Yassmin Kandeil, Ahmed Mostafa, Ahmed Ali, Mohamed A. Nossier, Eman S. Rasslan, Fatma Srour, Aladdin M. Sakhuja, Rajeev Ibrahim, Tarek S. Abdel-samii, Zakaria K.M. Al-Mahmoudy, Amany M.M. Bioorg Chem Article At present therapeutic options for severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) are very limited. We designed and synthesized three sets of small molecules using quinoline scaffolds. A series of quinoline conjugates (10a-l, 11a-c, and 12a-e) by incorporating 1,2,3-triazole were synthesized via a modified microwave-assisted click chemistry technique. Among the synthesized conjugates, 4-((1-(2-chlorophenyl)-1H-1,2,3-triazol-4-yl)methoxy)-6-fluoro-2-(trifluoromethyl)quinoline (10g) and 6-fluoro-4-(2-(1-(4-methoxyphenyl)-1H-1,2,3-triazol-4-yl)ethoxy)-2-(trifluoromethyl)quinoline (12c) show high potency against SARS-CoV-2. The selectivity index (SI) of compounds 10g and 12c also indicates the significant efficacy compared to the reference drugs. Elsevier Inc. 2021-09 2021-06-23 /pmc/articles/PMC8219945/ /pubmed/34214752 http://dx.doi.org/10.1016/j.bioorg.2021.105117 Text en © 2021 Elsevier Inc. 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 Seliem, Israa A. Panda, Siva S. Girgis, Adel S. Moatasim, Yassmin Kandeil, Ahmed Mostafa, Ahmed Ali, Mohamed A. Nossier, Eman S. Rasslan, Fatma Srour, Aladdin M. Sakhuja, Rajeev Ibrahim, Tarek S. Abdel-samii, Zakaria K.M. Al-Mahmoudy, Amany M.M. New quinoline-triazole conjugates: Synthesis, and antiviral properties against SARS-CoV-2 |
title | New quinoline-triazole conjugates: Synthesis, and antiviral properties against SARS-CoV-2 |
title_full | New quinoline-triazole conjugates: Synthesis, and antiviral properties against SARS-CoV-2 |
title_fullStr | New quinoline-triazole conjugates: Synthesis, and antiviral properties against SARS-CoV-2 |
title_full_unstemmed | New quinoline-triazole conjugates: Synthesis, and antiviral properties against SARS-CoV-2 |
title_short | New quinoline-triazole conjugates: Synthesis, and antiviral properties against SARS-CoV-2 |
title_sort | new quinoline-triazole conjugates: synthesis, and antiviral properties against sars-cov-2 |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8219945/ https://www.ncbi.nlm.nih.gov/pubmed/34214752 http://dx.doi.org/10.1016/j.bioorg.2021.105117 |
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