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

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.

Ar1 and/or Ar2 = heterocyclic ring (indole, benzothiophene, quinoleine, etc.); 3,4,5-(MeO)3C6H2CO; 3,4,5-(MeO)3C6H2CH2…Figure optionsDownload as PowerPoint slide