期刊
BIOORGANIC CHEMISTRY
卷 114, 期 -, 页码 -出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2021.105117
关键词
Quinoline; Triazole; Click chemistry; SARS-CoV-2; Molecular docking
资金
- Egyptian Cultural and Educational Bureau Scholarship
- Center for Undergraduate Research and Scholarship (CURS)
- Egyptian Academy of Scientific Research and Tech-nology (ASRT) [7303]
- Translational Research Program (TRP) at Augusta University
Novel small molecules with quinoline scaffolds were synthesized and assessed for their anti-SARS-CoV2 activity, with compounds 10g and 12c showing high potency and significant efficacy in comparison to reference drugs.
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-CoV2. The selectivity index (SI) of compounds 10g and 12c also indicates the significant efficacy compared to the reference drugs.
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