کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1392814 | 1501161 | 2012 | 8 صفحه PDF | دانلود رایگان |
Hexadecyloxypropyl esters of acyclic nucleoside phosphonates containing guanine (G) or hypoxanthine (Hx) and a (S)-[3-hydroxy-2-(phosphonomethoxy)propyl] [(S)-HPMP] or 2-(2-phosphonoethoxy)ethyl (PEE) acyclic moiety have been prepared. The activity of the prodrugs was evaluated in vitro against different virus families. Whereas ester derivatives of PEEHx and (S)-HPMPHx were antivirally inactive, monoesters of PEEG, and mono- and diesters of (S)-HPMPG showed pronounced antiviral activity against vaccinia virus and/or herpesviruses. Monoesters of (S)-HPMPG emerged as the most potent and selective derivatives against these DNA viruses. None of the compounds were inhibitory against RNA viruses and retroviruses.
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► Hexadecyloxypropyl prodrugs of (S)-HPMPG/Hx and PEEG/Hx were prepared.
► Their structures were confirmed through NMR and HRMS.
► The antiviral activity and cytotoxicity were screened in vitro.
► The cyclic monoester of (S)-HPMPG showed high antiviral activity and selectivity.
Journal: European Journal of Medicinal Chemistry - Volume 55, September 2012, Pages 307–314