University of Bechar, Algeria
Excessive levels of PAF and cells of macrophage lineage appear to play an important role in neuronal cell injury, inflammatory syndrome, and HIV replication in CNS resulting in AIDS dementia complex [1-4]. The beneficial effects of PAF receptor antagonists are evident and give rise to expected therapeutic strategies for neurotrauma. We therefore synthesized a novel class of 4-aminopiperidines and ethylenediamine substituted in the position 2 or 3 by groups bearing a carbamate or ureido function. Several substituents were introduced on one or both nitrogens of the 4-aminopiperidine and ethylenediamine rings in order to modify either lipophilicity, electronic distribution or steric effect [5]. Their influence on both anti-PAF and anti-HIV-1 activities was also investigated. Our findings revealed that the most compounds were found to be able to diminish both HIV-1 replication in monocyte-derived macrophages and PAF induced platelet aggregation. Moreover, a molecular modelling analysis has been triggered to calculate 3D electrostatic potential maps of selected compounds and to study the conformational space of the nitrogen-containing derivatives.
Pr BENMEHDI Houcine is a teacher in chemistry at TAHRI Mohamed University of Bechar since 2001, holder a doctorate degree in applied organic chemistry from Abou Bakr Belkaid University of Tlemcen, and a seconde doctorate degree in chemistry interfaces, physics, computer science with biology from Paris VII University in 2009. My field of research focused on phytochemistry, organic chemistry and environmental sciences.