title: Synthesis and anti-HIV activity of some novel lactyl and glycolyl phosphate derivatives.
abstract: Novel phosphate triester derivatives of 3'-acetylthymidine, and of the anti-HIV nucleoside analogue AZT have been prepared by phosphorochloridate chemistry. These materials are designed to act as membrane-soluble pro-drugs of the bio-active free nucleotides. In particular, novel glycolate and lactate phosphate derivatives have been prepared. In vitro evaluation revealed the AZT compounds to have a pronounced and selective antiviral effect, the magnitude of which varied considerably with the nature of the phosphate blocking group.
authors.affiliation: Department of Chemistry, University of Southampton, Highfield, U.K.
authors.forename: C
authors.initials: C
authors.lastname: McGuigan
authors.forename: C
authors.initials: C
authors.lastname: Nickson
authors.forename: T J
authors.initials: TJ
authors.lastname: O'Connor
authors.forename: D
authors.initials: D
authors.lastname: Kinchington
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D006678:HIV / Q000187:drug effects*; D009943:Organophosphorus Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D015215:Zidovudine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D000998:Antiviral Agents; D009943:Organophosphorus Compounds; D015215:Zidovudine