Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1366824 | Bioorganic & Medicinal Chemistry Letters | 2007 | 4 Pages |
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.
Graphical abstractGlycerolipidic prodrugs of didanosine 1 and didanosine monophosphate 2 were synthesized and evaluated against HIV-1 in cell culture with no sign of toxicity.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Muriel Lalanne, Angelo Paci, Karine Andrieux, Nathalie Dereuddre-Bosquet, Pascal Clayette, Alain Deroussent, Micheline Ré, Gilles Vassal, Patrick Couvreur, Didier Desmaële,