Prodrugs of HIV protease inhibitors-saquinavir, indinavir and nelfinavir-derived from diglycerides or amino acids: synthesis, stability and anti-HIV activity.

@article{Gaucher2004ProdrugsOH,
  title={Prodrugs of HIV protease inhibitors-saquinavir, indinavir and nelfinavir-derived from diglycerides or amino acids: synthesis, stability and anti-HIV activity.},
  author={B. Gaucher and M. Rouquayrol and D. Roche and J. Greiner and A. Aubertin and P. Vierling},
  journal={Organic \& biomolecular chemistry},
  year={2004},
  volume={2 3},
  pages={
          345-57
        }
}
With the aim of improving the pharmacological properties of current protease inhibitors (PIs), the synthesis of various acyl and carbamate amino acid- or diglyceride-containing prodrugs derived from saquinavir, indinavir and nelfinavir, their in vitro stability with respect to hydrolysis and their anti-HIV activity in CEM-SS and MT4 cells have been investigated. l-Leucine (Leu) and l-phenylalanine (Phe) were connected through their carboxyl to the PIs while l-tyrosine (Tyr) was conjugated… Expand
Investigation of oral bioavailability and brain distribution of the Ind(8)‐Val conjugate of indinavir in rodents
AMINO ACID TRANSPORTERS IN DRUG DISCOVERY
Prodrugs of Alcohols and Phenols
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