Structure-activity relationships in platelet-activating factor. Part 14: synthesis and biological evaluation of piperazine derivatives with dual anti-PAF and anti-HIV-1 activity

Wafa Sallem; Nawal Serradji; Nathalie Dereuddre-Bosquet; Georges Dive; Pascal Clayette; Françoise Heymans

doi:10.1016/j.bmc.2006.07.043

Structure-activity relationships in platelet-activating factor. Part 14: synthesis and biological evaluation of piperazine derivatives with dual anti-PAF and anti-HIV-1 activity

Bioorg Med Chem. 2006 Dec 1;14(23):7999-8013. doi: 10.1016/j.bmc.2006.07.043.

Authors

Wafa Sallem¹, Nawal Serradji, Nathalie Dereuddre-Bosquet, Georges Dive, Pascal Clayette, Françoise Heymans

Affiliation

¹ 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.

PMID: 16908170
DOI: 10.1016/j.bmc.2006.07.043

Abstract

As HIV-associated dementia prevalence has risen with the lifespan of HIV-infected individuals, there is an important need for antiretroviral and anti-inflammatory drugs targeting the central nervous system. Platelet-activating factor, a mediator of inflammation, is an HIV-induced neurotoxin secreted in the infected brain. In this work, we developed piperazine derivatives bearing a heterocyclic moiety as PAF-antagonists and HIV-1 replication inhibitors with micromolar potency.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Acquired Immunodeficiency Syndrome / complications*
Anti-HIV Agents / chemical synthesis*
Anti-HIV Agents / pharmacology
Dementia / etiology
Dementia / prevention & control*
Dose-Response Relationship, Drug
HIV-1
Humans
Piperazines / chemical synthesis
Piperazines / pharmacology*
Platelet Activating Factor / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Anti-HIV Agents
Piperazines
Platelet Activating Factor