Synthesis and HIV-1 reverse transcriptase inhibition properties of two new methylenephosphonate analogues of 3′-azido-3′-deoxythymidine-5′-triphosphate
| Autor: | Patrick Labataille, H. Pelicano, Georges Maury, Gilles Gosselin, Jean Louis Imbach |
|---|---|
| Rok vydání: | 1995 |
| Předmět: |
chemistry.chemical_classification
3'-azido-3'-deoxythymidine 5'-triphosphate viruses Organic Chemistry Clinical Biochemistry Human immunodeficiency virus (HIV) virus diseases Pharmaceutical Science biochemical phenomena metabolism and nutrition medicine.disease_cause Biochemistry Reverse transcriptase chemistry.chemical_compound Enzyme chemistry immune system diseases Drug Discovery medicine Molecular Medicine heterocyclic compounds Methylene Molecular Biology |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 5:2315-2320 |
| ISSN: | 0960-894X |
| Popis: | Two new 5′-phosphorylated derivatives of 3′-azido-3′-deoxythymidine (AZT), namely α,β;β,γ-bis (methylene) AZT-5′-triphosphate 1 and α,β-propylene AZT 5′-diphosphate 2 , were synthesized. When evaluated for their inhibitory effects on human immunodeficiency virus (HIV) reverse transcriptase, these compounds were about 1000-fold less active than AZT-5′-triphosphate (AZTTP) as competitive inhibitors of this enzyme. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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