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Development of ciclesonide analogues that block SARS-CoV-2 RNA replication
Genichiro Tsuji1, Kenzo Yonemitsu2, Takahito Ito1
1Division of Organic Chemistry, National Institute of Health Sciences, 3-25-26, Tonomachi, Kawasaki, Kanagawa 210-9501, Japan.
Bioorganic & Medicinal Chemistry Letters
|April 22, 2021
Summary
New ciclesonide analogues, Cic4 and Cic6, show potent antiviral activity against SARS-CoV-2, offering promising therapeutic potential for COVID-19 treatment. These compounds effectively repressed viral replication with low cytotoxicity.
Area of Science:
- Pharmacology
- Virology
- Medicinal Chemistry
Background:
- Ciclesonide, an inhaled corticosteroid for asthma, is being investigated for COVID-19 treatment.
- An active metabolite, Cic2, demonstrated repression of SARS-CoV-2 replication.
Purpose of the Study:
- To design and synthesize novel ciclesonide analogues.
- To evaluate the antiviral activity and cytotoxicity of these analogues against SARS-CoV-2.
Main Methods:
- Synthesis of ciclesonide analogues, including Cic4 (azide group) and Cic6 (chloro group).
- Assessment of antiviral efficacy against SARS-CoV-2 replication.
- Evaluation of cytotoxicity of the synthesized compounds.
Main Results:
- Cic4 and Cic6 analogues potently decreased SARS-CoV-2 viral replication.
- These analogues exhibited low cytotoxicity compared to Cic2.
- Significant antiviral activity was observed in the novel compounds.
Conclusions:
- Ciclesonide analogues Cic4 and Cic6 demonstrate significant potential as novel therapeutic agents for COVID-19.
- The compounds show promising antiviral activity and favorable safety profiles.
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