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 |
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| Authors: | Serradji Nawal Bensaid Okkacha Martin Marc Sallem Wafa Dereuddre-Bosquet Nathalie Benmehdi Houcine Redeuilh Catherine Lamouri Aazdine Dive Georges Clayette Pascal Heymans Françoise |
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| Institution: | Unité de Recherche Pharmacochimie Moléculaire et Systèmes Membranaires (EA 2381), Laboratoire de Pharmacochimie Moléculaire, Université Paris 7 - Denis Diderot, case 7066, 2 Place Jussieu, 75251 Paris Cedex 05, France. serradji@paris7.jussieu.fr |
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| Abstract: | 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. |
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