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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
  • 5
    Citations
  • 0
    Usage
  • 10
    Captures
  • 1
    Mentions
  • 0
    Social Media
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  • Citations
    5
  • Captures
    10
  • Mentions
    1
    • News Mentions
      1
      • 1

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

Shin, Young Sup; Lee, Jun Young; Jeon, Sangeun; Myung, Subeen; Gong, Hyun June; Kim, Seungtaek; Kim, Hyoung Rae; Jeong, Lak Shin; Park, Chul Min

Elsevier BV

Biochemistry, Genetics and Molecular Biology; Pharmacology, Toxicology and Pharmaceutics; Chemistry

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