Synthesis and biological evaluation of two glycerolipidic prodrugs of didanosine for direct lymphatic delivery against HIV

Muriel Lalanne, Angelo Paci, Karine Andrieux, Nathalie Dereuddre-Bosquet, Pascal Clayette, Alain Deroussent, Micheline Ré, Gilles Vassal, Patrick Couvreur, Didier Desmaële

Résultats de recherche: Contribution à un journalArticleRevue par des pairs

35 Citations (Scopus)

Résumé

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.

langue originaleAnglais
Pages (de - à)2237-2240
Nombre de pages4
journalBioorganic and Medicinal Chemistry Letters
Volume17
Numéro de publication8
Les DOIs
étatPublié - 15 avr. 2007
Modification externeOui

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