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Details

Autor(en) / Beteiligte
Titel
Synthesis and biological evaluation of two glycerolipidic prodrugs of didanosine for direct lymphatic delivery against HIV
Ist Teil von
  • Bioorganic & medicinal chemistry letters, 2007-04, Vol.17 (8), p.2237-2240
Ort / Verlag
Oxford: Elsevier Ltd
Erscheinungsjahr
2007
Link zum Volltext
Quelle
Elsevier ScienceDirect Journals Complete
Beschreibungen/Notizen
  • Glycerolipidic prodrugs of didanosine 1 and didanosine monophosphate 2 were synthesized and evaluated against HIV-1 in cell culture with no sign of toxicity. 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.

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