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Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Bioorg+Chem 2021 ; 114 (ä): 105117 Nephropedia Template TP
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New quinoline-triazole conjugates: Synthesis, and antiviral properties against SARS-CoV-2 #MMPMID34214752
Seliem IA; Panda SS; Girgis AS; Moatasim Y; Kandeil A; Mostafa A; Ali MA; Nossier ES; Rasslan F; Srour AM; Sakhuja R; Ibrahim TS; Abdel-Samii ZKM; Al-Mahmoudy AMM
Bioorg Chem 2021[Sep]; 114 (ä): 105117 PMID34214752show ga
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.