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

Lalanne M, Paci A, Andrieux K, Dereuddre-Bosquet N, Clayette P, Deroussent A, Ré M, Vassal G, Couvreur P, Desmaële D

Université Paris-Sud, UMR CNRS 8612, IFR 141, F-92296 Châtenay-Malabry, France.

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.

Published 2 April 2007 in Bioorg Med Chem Lett, 17(8): 2237-40.
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