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  • Title: Phosphoramidate derivatives of acyclovir: synthesis and antiviral activity in HIV-1 and HSV-1 models in vitro.
    Author: Zakirova NF, Shipitsyn AV, Jasko MV, Prokofjeva MM, Andronova VL, Galegov GA, Prassolov VS, Kochetkov SN.
    Journal: Bioorg Med Chem; 2012 Oct 01; 20(19):5802-9. PubMed ID: 22954898.
    Abstract:
    The antiviral activity against HIV and HSV and the chemical stability of ACV phosphoramidate derivatives were studied. The phosphoramidates of ACV demonstrated moderate activity. The best compound appeared to be 9-(2-hydroxymethyl)guanine phosphoromonomorpholidate (7), which inhibited virus replication in pseudo-HIV-1 particles by 50% at 50 μM. It also inhibited replication of wild-type HSV-1 (9.7 μM) as well as an acyclovir-resistant strain (25 μM). None of the synthesised compounds showed any cytotoxicity.
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