Amidate Prodrugs of O‑2-Alkylated
Pyrimidine Acyclic Nucleosides Display Potent Anti-Herpesvirus Activity

Herdewijn, Piet

Amidate Prodrugs of O‑2-Alkylated Pyrimidine Acyclic Nucleosides Display Potent Anti-Herpesvirus Activity

Posted on 2020-06-24 - 18:37

Three series of amidate prodrugs of O-2-alkylated acyclic nucleosides of the 3-fluoro-2-(phosphonomethoxy)propyl (FPMP), cyclic 3-hydroxy-2-(phosphonomethoxypropyl) (cHPMP), and 2-(phosphonomethoxypropyl) (PMP)-type featuring cytosine and 5-fluorocytosine as nucleobases were readily synthesized. Both the aspartic acid ester and valine ester prodrugs of (R)-O-2-alkylated FPMPC exhibited potent anti-HCMV and VZV activity in the micromolar range. In addition, the valine ester prodrugs of 5-fluorocytosine (R)-O-2-alkylated FPMP and (R)-O-2-alkylated cHPMPC showed inhibitory activity at molar concentrations against these viruses.

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Luo, Min; Groaz, Elisabetta; Snoeck, Robert; Andrei, Graciela; Herdewijn, Piet (2020). Amidate Prodrugs of O‑2-Alkylated Pyrimidine Acyclic Nucleosides Display Potent Anti-Herpesvirus Activity. ACS Publications. Collection. https://doi.org/10.1021/acsmedchemlett.0c00090

https://doi.org/10.1021/acsmedchemlett.0c00090

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