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New quinoline-triazole conjugates: Synthesis, and antiviral properties against SARS-CoV-2.
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.
  • Seliem IA; Department of Chemistry and Physics, Augusta University, Augusta, GA 30912, USA; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt.
  • Panda SS; Department of Chemistry and Physics, Augusta University, Augusta, GA 30912, USA. Electronic address: sipanda@augusta.edu.
  • Girgis AS; Department of Pesticide Chemistry, National Research Centre, Dokki, Giza 12622, Egypt.
  • Moatasim Y; Center of Scientific Excellence for Influenza Viruses, National Research Centre, Giza 12622, Egypt.
  • Kandeil A; Center of Scientific Excellence for Influenza Viruses, National Research Centre, Giza 12622, Egypt.
  • Mostafa A; Center of Scientific Excellence for Influenza Viruses, National Research Centre, Giza 12622, Egypt.
  • Ali MA; Center of Scientific Excellence for Influenza Viruses, National Research Centre, Giza 12622, Egypt.
  • Nossier ES; Department of Pharmaceutical Medicinal Chemistry and Drug Design, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt.
  • Rasslan F; Department of Microbiology and Immunology, Faculty of Pharmacy (Girls), Al Azhar University, Cairo, Egypt.
  • Srour AM; Department of Therapeutic Chemistry, National Research Centre, Dokki, Giza 12622, Egypt.
  • Sakhuja R; Department of Chemistry, Birla Institute of Technology and Science, Pilani, India.
  • Ibrahim TS; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
  • Abdel-Samii ZKM; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt.
  • Al-Mahmoudy AMM; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt.
Bioorg Chem ; 114: 105117, 2021 09.
Article in English | MEDLINE | ID: covidwho-1283943
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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Full text: Available Collection: International databases Database: MEDLINE Main subject: Antiviral Agents / Quinolines / Triazoles / COVID-19 Drug Treatment Limits: Humans Language: English Journal: Bioorg Chem Year: 2021 Document Type: Article Affiliation country: J.bioorg.2021.105117

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Full text: Available Collection: International databases Database: MEDLINE Main subject: Antiviral Agents / Quinolines / Triazoles / COVID-19 Drug Treatment Limits: Humans Language: English Journal: Bioorg Chem Year: 2021 Document Type: Article Affiliation country: J.bioorg.2021.105117