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

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Discovery of an L-like Configuration for 3’-Fluoro-5’-norcarbonucleoside Phosphonates as Potent Anti-HIV Agents
ChemMedChem ( IF 3.6 ) Pub Date : 2022-08-29 , DOI: 10.1002/cmdc.202200377
Pierre-Yves Geant ₁ , Malika Kaci ₁ , Jean-Pierre Uttaro ₁ , Christian Périgaud ₁ , Christophe Mathé ₁

Affiliation

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.

中文翻译：

发现 3'-Fluoro-5'-norcarbonucleoside 磷酸盐的 L 样构型作为有效的抗 HIV 药物

我们最近报道了以腺嘌呤为杂环碱基的 3'-fluoro-5'-norcarbocyclic nucleoside phosphonates 的外消旋合成。为了评估每种对映体的抗病毒活性，我们合成了两种对映体及其相应的双 (POM) 前药。介绍了针对 HIV-1 LAI 菌株和临床 NRTI 抗性 HIV-1 菌株的评估。针对这些不同菌株的活性表明，双 (POM) 前药 (−)- 9的活性等同于甚至优于 ( R)- PMPA。

更新日期：2022-08-29

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