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Updated: Jul 9, 2026
15:22
Nucleoside Triphosphates - From Synthesis to Biochemical Characterization
Published on: April 3, 2014
Some novel aminopropyl nucleoside phosphonates.
Ding Zhou1, Irene M Lagoja, Arthur Van Aerschot
1Laboratory of Medicinal Chemistry, Rega Institute, Leuven, Belgium.
Nucleosides, Nucleotides & Nucleic Acids
|December 11, 2007
Summary
Aminopropyl nucleoside phosphonates were synthesized as analogs of Cidofovir (HPMPC). While some compounds showed potential, only weak antiherpes virus activity was observed for specific analogs.
Area of Science:
- Medicinal Chemistry
- Virology
- Organic Synthesis
Background:
- HPMPC (Cidofovir) is an antiviral drug.
- Nucleoside phosphonates are a class of antiviral agents.
- Modifications to nucleoside analogs can alter antiviral activity.
Purpose of the Study:
- To synthesize novel aminopropyl nucleoside phosphonates.
- To evaluate the antiherpes virus activity of these new compounds.
- To compare their activity to HPMPC.
Main Methods:
- Synthesis of purine and pyrimidine nucleoside analogs.
- Incorporation of an aminopropyl group into the acyclic chain or as a substituent.
- Antiviral activity testing against herpes viruses.
Main Results:
- Aminopropyl nucleoside phosphonates (compounds 1-3) were successfully synthesized.
- Compounds 2b and 2c, with amino functions in the acyclic chain, showed only weak antiherpes virus activity.
- Activity was significantly less potent compared to HPMPC.
Conclusions:
- The introduction of an aminopropyl group in these positions did not enhance antiherpes virus activity.
- Further structural modifications may be needed to develop potent antiviral agents in this series.
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