Author/Authors :
Muriel Lalanne، نويسنده , , Angelo Paci، نويسنده , , Karine Andrieux، نويسنده , , Nathalie Dereuddre-Bosquet، نويسنده , , Pascal Clayette، نويسنده , , Alain Deroussent، نويسنده , , Micheline Ré، نويسنده , , Gilles Vassal، نويسنده , , Patrick Couvreur ، نويسنده , , Didier Desmaële، نويسنده ,
Abstract :
Novel glycerolipidic prodrugs of didanosine and didanosine monophosphate designed to by-pass the hepatic first pass metabolism were synthesized and tested for their cytotoxicity and anti-HIV-1 activity. Formulation as liposomes of dipalmitoylphosphatidylcholine was elaborated. A simple quantitative HPLC-UV method was developed and validated, and ESI-MS was used for qualitative purpose. These two prodrugs exhibited promising biological activities against HIV-1 in in vitro infected cell culture.
Keywords :
Anti-HIV nucleoside , Lipid–nucleoside conjugate , prodrugs , Enzyme inhibitors , bioavailability
