Synthesis and Anti-HIV Activity of Some Heterodimers [NRTI]-Glycyl-Succinyl-[Trovirdine Analogue] of Known HIV-1 Reverse Transcriptase Inhibitors
| Autor: | Anne-Marie Aubertin, E. Sugeac, Sylvie Schmidt, D. Laduree, Christine Fossey, Geraldine Laumond |
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| Rok vydání: | 2003 |
| Předmět: |
Anti-HIV Agents
Pyridines Glycine Succinic Acid Human immunodeficiency virus (HIV) medicine.disease_cause Cell Line Nucleoside Reverse Transcriptase Inhibitor Inhibitory Concentration 50 Structure-Activity Relationship immune system diseases Drug Discovery medicine Humans Moiety Structure–activity relationship Pharmacology Molecular Structure Reverse-transcriptase inhibitor Chemistry virus diseases General Medicine biochemical phenomena metabolism and nutrition Virology HIV Reverse Transcriptase Reverse transcriptase Trovirdine HIV-1 Reverse Transcriptase Inhibitors Dimerization Linker medicine.drug |
| Zdroj: | Journal of Enzyme Inhibition and Medicinal Chemistry. 18:175-186 |
| ISSN: | 1475-6374 1475-6366 |
| Popis: | Expected for their ability to inhibit HIV replication, four heterodimers with a Nucleoside Reverse Transcriptase Inhibitor (NRTI) and a Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) bound by a linker arm were designed and synthesized. For the NRTIs, d4U, d2U, d4T and 5'-O-acetyl-5-(3-hydroxypropynyl)d2U were chosen. For the NNRTI, a Trovirdine Analogue (belonging to the phenethylthiazolylthiourea class) was chosen. The conjugation of the two different inhibitors (NRTI and NNRTI) was performed using the succinyl-glycine moiety as a spontaneously cleavable linker. |
| Databáze: | OpenAIRE |
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