Discovery of 2-aminoquinolone acid derivatives as potent inhibitors of SARS-CoV-2
Bioorganic & Medicinal Chemistry Letters, ISSN: 0960-894X, Vol: 85, Page: 129214
2023
- 5Citations
- 10Captures
- 1Mentions
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Most Recent News
New Findings from Seoul National University Describe Advances in COVID-19 (Discovery of 2-aminoquinolone Acid Derivatives As Potent Inhibitors of Sars-cov-2)
2023 APR 26 (NewsRx) -- By a News Reporter-Staff News Editor at NewsRx COVID-19 Daily -- Research findings on Coronavirus - COVID-19 are discussed in
Article Description
The COVID-19 pandemic caused by the Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) continues to threaten human health and create socioeconomic problems worldwide. A library of 200,000 small molecules from the Korea Chemical Bank (KCB) were evaluated for their inhibitory activities against SARS-CoV-2 in a phenotypic-based screening assay to discover new therapeutics to combat COVID-19. A primary hit of this screen was the quinolone structure-containing compound 1. Based on the structure of compound 1 and enoxacin, which is a quinolone-based antibiotic previously reported to have weak activity against SARS-CoV-2, we designed and synthesized 2-aminoquinolone acid derivatives. Among them, compound 9b exhibited potent antiviral activity against SARS-CoV-2 (EC 50 = 1.5 µM) without causing toxicity, while having satisfactory in vitro PK profiles. This study shows that 2-aminoquinolone acid 9b provides a promising new template for developing anti-SARS-CoV-2 entry inhibitors.
Bibliographic Details
http://www.sciencedirect.com/science/article/pii/S0960894X23000926; http://dx.doi.org/10.1016/j.bmcl.2023.129214; http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85149637212&origin=inward; http://www.ncbi.nlm.nih.gov/pubmed/36870624; https://linkinghub.elsevier.com/retrieve/pii/S0960894X23000926; https://dx.doi.org/10.1016/j.bmcl.2023.129214
Elsevier BV
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