| Autor: |
McGuigan, C., Bellevergue, P., Jones, B. C. N. M., Mahmood, N., Hay, A. J., Petrik, J., Karpas, A. |
| Zdroj: |
Antiviral Chemistry & Chemotherapy; August 1994, Vol. 5 Issue: 4 p271-277, 7p |
| Abstrakt: |
Novel alkyl hydrogen phosphonate derivatives of the anti-HIV nucleoside analogue AZT have been prepared by phosphorochloridite chemistry. These materials are designed to act as labile membrane-soluble prodrugs of the bioactive free nucleotides. In vitroevaluation has revealed the compounds to have a pronounced and selective antiviral action. Short-chain (C1-C7) alkyl derivatives are more potent than the parent hydrogen phosphonate, whilst one long-chain (C18) compound is less active. In an assay that demonstrates the toxicity of the parent drug AZT, the alkyl H-phosphonates appear to be less cytotoxic, whilst retaining full antiviral activity. Lastly, the compounds are all poorly active in a cell line (JM) that is poorly responsive to AZT, indicating that they act as depot forms of the nucleoside rather than of the free nucleotide. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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