Synthesis and evaluation of enantiomers of hydroxychloroquine against SARS-CoV-2 in vitro.
Bioorg Med Chem
; 53: 116523, 2022 01 01.
Article
in English
| MEDLINE | ID: covidwho-1525708
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.
Keywords
Full text:
Available
Collection:
International databases
Database:
MEDLINE
Main subject:
Antiviral Agents
/
SARS-CoV-2
/
Hydroxychloroquine
Type of study:
Experimental Studies
Limits:
Animals
Language:
English
Journal:
Bioorg Med Chem
Journal subject:
Biochemistry
/
Chemistry
Year:
2022
Document Type:
Article
Affiliation country:
J.bmc.2021.116523
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