Synthesis and Evaluation of Some Novel Phosphoramidate Derivatives of 3′-Azido-3′-Deoxythymidine (AZT) as Anti-HIV Compounds
| Autor: | Kevin G. Devine, D.J. Jeffries, D. Kinchington, T. J. O'Connor, S. A. Galpin, C. McGuigan |
|---|---|
| Rok vydání: | 1990 |
| Předmět: |
0301 basic medicine
chemistry.chemical_classification Stereochemistry 030106 microbiology Phosphoramidate Biological activity General Medicine Prodrug Biology 01 natural sciences In vitro 0104 chemical sciences Amino acid 010404 medicinal & biomolecular chemistry 03 medical and health sciences chemistry Moiety Nucleotide Alkyl |
| Zdroj: | Antiviral Chemistry and Chemotherapy. 1:107-113 |
| ISSN: | 2040-2066 |
| Popis: | A series of monophosphate triester derivatives of 3′-azido-3′-deoxythymidine (AZT), designed as membrane-soluble pro-drugs of the nucleotide (AZTMP), have been tested for activity against the human immunodeficiency virus (HIV-1). It has been found that when carboxyl-protected, amino-linked amino acids, and alkyl chains, are asymmetrically substituted on the 5′-phosphate a significant antiviral effect is observed. Moreover, the activity of the compounds is profoundly dependent on the structure of the phosphate moiety, and in particular on the nature of the amino acid. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|