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...

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Detalles Bibliográficos
Autores principales: 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.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Inc. 2021
Materias:
Article
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
Descripción
Sumario: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.

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