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Synthesis of peptide analogues containing phosphonamidate methyl ester functionality: HIV-1 proteinase inhibitors possessing unique cell uptake properties
- Source :
- Bioorganicmedicinal chemistry. 3(3)
- Publication Year :
- 1995
-
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.
- Subjects :
- Stereochemistry
Clinical Biochemistry
Cell
Molecular Sequence Data
Human immunodeficiency virus (HIV)
Organophosphonates
Pharmaceutical Science
Peptide
medicine.disease_cause
Virus Replication
Biochemistry
Virus
Drug Discovery
medicine
Ic50 values
Amino Acid Sequence
Molecular Biology
chemistry.chemical_classification
Molecular Structure
Chemistry
Organic Chemistry
Esters
Stereoisomerism
HIV Protease Inhibitors
Enzyme inhibition
medicine.anatomical_structure
HIV-1
Molecular Medicine
Peptides
Subjects
Details
- ISSN :
- 09680896
- Volume :
- 3
- Issue :
- 3
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry
- Accession number :
- edsair.doi.dedup.....fb9154538d915074c91512f01967092f