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

Faculty Pharmacy Year: 2021
Type of Publication: ZU Hosted Pages:
Authors:
Israa Abdallah Mostafa Sliem
Journal: Bioorganic Chemistry Elsevier Volume:
Keywords : , quinoline-triazole conjugates: Synthesis, , antiviral properties against    
Abstract:
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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