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

Israa A. Seliem, Siva S. Panda, Adel S. Girgis, Yassmin Moatasim, Ahmed Kandeil, Ahmed Mostafa, Mohamed A. Ali, Eman S. Nossier, Fatma Rasslan, Aladdin M. Srour, Rajeev Sakhuja, Tarek S. Ibrahim, Zakaria K.M. Abdel-samii, Amany M.M. Al-Mahmoudy

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish (US)
Article number105117
JournalBioorganic Chemistry
Volume114
DOIs
StatePublished - Sep 2021

Keywords

  • Click chemistry
  • Molecular docking
  • Quinoline
  • SARS-CoV-2
  • Triazole

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Drug Discovery
  • Organic Chemistry

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