Structure–activity relationships in platelet-activating factor. Part 13: Synthesis and biological evaluation of piperazine derivatives with dual anti-PAF and anti-HIV-1 or pure antiretroviral activity
| Autor: | Nathalie Dereuddre-Bosquet, Françoise Heymans, Wafa Sallem, Catherine Redeuilh, Nawal Serradji, Houcine Benmehdi, Marc Martin, Georges Dive, Okkacha Bensaid, Aazdine Lamouri, Pascal Clayette |
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| Rok vydání: | 2006 |
| Předmět: |
Molecular model
Anti-HIV Agents Clinical Biochemistry AIDS-related complex Pharmaceutical Science Pharmacology Biochemistry Chemical synthesis Piperazines Structure-Activity Relationship chemistry.chemical_compound Drug Discovery medicine Humans Platelet Activating Factor Molecular Biology Acquired Immunodeficiency Syndrome Dose-Response Relationship Drug biology Platelet-activating factor Chemistry Organic Chemistry Neurotoxicity biology.organism_classification medicine.disease Piperazine Anti-Retroviral Agents Viral replication Lentivirus HIV-1 Molecular Medicine Dementia |
| Zdroj: | Bioorganic & Medicinal Chemistry. 14:8109-8125 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2006.07.031 |
| Popis: | HIV-1 infection of the brain and PAF neurotoxicity are implicated in AIDS dementia complex. We previously reported that a trisubstituted piperazine derivative is able to diminish both HIV-1 replication in monocyte-derived macrophages and PAF-induced platelet aggregation. We report in this work new compounds obtained by modifying its piperazine substituents. The structure-activity relationship study shows that a better dual activity or even pure antiretroviral compounds can be obtained in this series. |
| Databáze: | OpenAIRE |
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