title: Phosphoramidate derivatives of acyclovir: synthesis and antiviral activity in HIV-1 and HSV-1 models in vitro.
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.
authors.affiliation: Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, 32 Vavilov St., Moscow, 119991, Russian Federation. naucik@aport2000.ru
authors.forename: Natalia F
authors.initials: NF
authors.lastname: Zakirova
authors.forename: Alexander V
authors.initials: AV
authors.lastname: Shipitsyn
authors.forename: Maxim V
authors.initials: MV
authors.lastname: Jasko
authors.forename: Maria M
authors.initials: MM
authors.lastname: Prokofjeva
authors.forename: Valeria L
authors.initials: VL
authors.lastname: Andronova
authors.forename: Georgiy A
authors.initials: GA
authors.lastname: Galegov
authors.forename: Vladimir S
authors.initials: VS
authors.lastname: Prassolov
authors.forename: Sergey N
authors.initials: SN
authors.lastname: Kochetkov
mesh_terms: D000212:Acyclovir / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D057809:HEK293 Cells; D015658:HIV Infections / Q000188:drug therapy; D015497:HIV-1 / Q000187:drug effects*; D006561:Herpes Simplex / Q000188:drug therapy; D018259:Herpesvirus 1, Human / Q000187:drug effects*; D006801:Humans; D014709:Vero Cells; D014779:Virus Replication / Q000187:drug effects
chemical_list: D000998:Antiviral Agents; D000212:Acyclovir