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Discovery of an L‐like Configuration for 3’‐Fluoro‐5’‐norcarbonucleoside Phosphonates as Potent Anti‐HIV Agents

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We recently reported the racemic synthesis of 3’-fluoro-5’-norcarbocyclic nucleoside phosphonates bearing adenine as heterocyclic base. To evaluate the antiviral activity of each enantiomer, we synthesized both enantiomers as well as their corresponding bis(POM) prodrugs. Evaluations against the HIV-1 LAI strain and clinically NRTI-resistant HIV-1 strains are presented. The activities against these different strains show that the activities of bis(POM) prodrug (−)-9 are equivalent or even superior to those of (R)-PMPA.


Abstract

Recently, we reported the racemic synthesis of 3’-fluoro-5’-norcarbocyclic nucleoside phosphonates bearing adenine as the heterocyclic base. For this study, to evaluate the antiviral activity of each enantiomer, we synthesized both enantiomers, as well as their corresponding bis(POM) prodrugs. Anti-HIV-1 evaluation against the LAI strain and clinically NRTI-resistant HIV-1 strains are presented. The activities against these different strains show that the activities of bis(POM) prodrug (−)-9 are equivalent or even superior to those of (R)-PMPA.

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