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5'-Nor-3-Deaza-1',6'-Isoneplanocin, the Synthesis and Antiviral Study
Qi Chen1, Stewart W Schneller2, Chong Liu2
1Department of Chemistry, Slippery Rock University, Slippery Rock, PA 16057, USA.
Molecules (Basel, Switzerland)
|August 29, 2020
Summary
Researchers developed a novel synthesis for C-5'-truncated 3-deaza-1',6'-isoneplanocin, yielding compounds with potent antiviral activity against JC virus but not other viruses. These new antiviral agents demonstrated no cytotoxicity.
Area of Science:
- Medicinal Chemistry
- Virology
- Organic Synthesis
Background:
- Aristeromycin and neplanocin are arbocyclic nucleosides investigated for antiviral properties.
- Developing novel antiviral agents remains a critical area in pharmaceutical research.
Purpose of the Study:
- To synthesize C-5 truncated 3-deaza-1 6 -isoneplanocin, combining structural features of 5 -noraristeromycin and 3-deaza-1 6 -isoneplanocin.
- To evaluate the antiviral activity and cytotoxicity of the synthesized compounds.
Main Methods:
- A convenient synthesis route starting from (-)-cyclopentenone.
- Preparation of the two C-4 epimers of 5 -nor-3-deaza isoneplanocin.
- Antiviral assays against JC virus and other DNA/RNA viruses.
- Cytotoxicity assays.
Main Results:
- The synthesis yielded two epimers of 5 -nor-3-deaza isoneplanocin.
- One epimer ((4 'R)-8) showed significant activity against JC virus (EC50 = 1.12 µM).
- Both compounds were inactive against other tested DNA and RNA viruses and exhibited no cytotoxicity.
Conclusions:
- The synthesized C-5 -truncated 3-deaza-1 6 -isoneplanocin derivatives are promising candidates for JC virus treatment.
- Further research may explore modifications to broaden the antiviral spectrum.
- The lack of cytotoxicity is a favorable characteristic for potential therapeutic applications.
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