ArticleBioorganic & medicinal chemistry2022
Synthesis and evaluation of enantiomers of hydroxychloroquine against SARS-CoV-2 in vitro.
Article in Bioorganic & medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed.
- Antiviral Activity of Essential Oil fromMolecules (Basel, Switzerland) · 2026Article
- A NewPharmaceuticals (Basel, Switzerland) · 2025Article
- Hydroxychloroquine's diverse targets: a new frontier in precision medicine.Frontiers in immunology · 2025Review
- Dissimilar effects of stereoisomers and racemic hydroxychloroquine on CaPhysiological reports · 2023Article
- Review
- Multi-target activity of copper complexes: Antibacterial, DNA binding, and molecular docking with SARS-CoV-2 receptor.Chemico-biological interactions · 2023Article
- Neutrophil Immunomodulatory Activity of (-)-Borneol, a Major Component of Essential Oils Extracted fromMolecules (Basel, Switzerland) · 2022Article
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Authors and funding
8 authors.
Funding
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Abstract
Since the end of 2019, the outbreak of Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) has evolved into a global pandemic. There is an urgent need for effective and low-toxic antiviral drugs to remedy Remdesivir's limitation. Hydroxychloroquine, a broad spectrum anti-viral drug, showed inhibitory activity against SARS-CoV-2 in some studies. Thus, we adopted a drug repurposing strategy, and further investigated hydroxychloroquine. We obtained different configurations of hydroxychloroquine side chains by using chiral resolution technique, and successfully furnished R-/S-hydroxychloroquine sulfate through chemical synthesis. The R configuration of hydroxychloroquine was found to exhibit higher antiviral activity (EC50 = 3.05 μM) and lower toxicity in vivo. Therefore, R-HCQ is a promising lead compound against SARS-CoV-2. Our research provides new strategy for the subsequent research on small molecule inhibitors against SARS-CoV-2.
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