New quinoline-triazole conjugates: Synthesis, and antiviral properties against SARS-CoV-2

A series of quinolone-triazole conjugates synthesized as potential antiviral agents for SARS-CoV2. Some of the conjugates are more potent than the standards. [Display omitted] •A set of quinolone-triazole conjugates was designed and synthesized.•Some conjugates show promising antiviral properties ag...

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Bibliographic Details
Published in:Bioorganic chemistry 2021-09, Vol.114, p.105117-105117, Article 105117
Main Authors: 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.
Format: Article
Language:English
Subjects:
Antiviral Agents - chemical synthesis
Antiviral Agents - chemistry
Click Chemistry
COVID-19 Drug Treatment
Humans
Molecular docking
Molecular Docking Simulation
Quinoline
Quinolines - chemical synthesis
Quinolines - chemistry
SARS-CoV-2
Triazole
Triazoles - chemical synthesis
Triazoles - chemistry
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Summary:A series of quinolone-triazole conjugates synthesized as potential antiviral agents for SARS-CoV2. Some of the conjugates are more potent than the standards. [Display omitted] •A set of quinolone-triazole conjugates was designed and synthesized.•Some conjugates show promising antiviral properties against SARS-CoV2.•The selectivity index (SI) of the synthesized potent conjugates better than the reference drugs.•Potential conjugates could be further explored for the development of potential antiviral drug candidates. 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.
ISSN:0045-2068
1090-2120
DOI:10.1016/j.bioorg.2021.105117