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.
Sallem
Wafa
W
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
Nawal
N
Dereuddre-Bosquet
Nathalie
N
Dive
Georges
G
Clayette
Pascal
P
Heymans
Françoise
F
D000163:Acquired Immunodeficiency Syndrome / Q000150:complications*; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D003704:Dementia / Q000209:etiology / Q000517:prevention & control*; D004305:Dose-Response Relationship, Drug; D015497:HIV-1; D006801:Humans; D010879:Piperazines / Q000138:chemical synthesis / Q000494:pharmacology*; D010972:Platelet Activating Factor / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D019380:Anti-HIV Agents; D010879:Piperazines; D010972:Platelet Activating Factor