Synthesis of peptide analogues containing phosphonamidate methyl ester functionality: HIV-1 proteinase inhibitors possessing unique cell uptake properties Original Research Article

Synthesis of peptide analogues containing phosphonamidate methyl ester functionality: HIV-1 proteinase inhibitors possessing unique cell uptake properties Original Research Article Pages 297-312 Nicholas P. Camp, David A. Perrey, Derek Kinchington, Paul C.D. Hawkins, David Gani Close preview | Related articles | Related reference work articles Abstract | References Abstract Stereochemically defined and epimeric phosphonamidate methyl ester-containing peptide analogues were synthesised and were found to be moderate inhibitors of the HIV-1 proteinase. All of the analogues containing the phosphonamidate ester grouping showed a marked ability to enter cells, as highlighted by the approximate equivalence of the IC50 values for enzyme inhibition in solution and inhibition of HIV-1 replication in virus infected cells.