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.
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.
Serradji
Nawal
N
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
Bensaid
Okkacha
O
Martin
Marc
M
Sallem
Wafa
W
Dereuddre-Bosquet
Nathalie
N
Benmehdi
Houcine
H
Redeuilh
Catherine
C
Lamouri
Aazdine
A
Dive
Georges
G
Clayette
Pascal
P
Heymans
Françoise
F
D000163:Acquired Immunodeficiency Syndrome / Q000150:complications*; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D044966:Anti-Retroviral 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; D044966:Anti-Retroviral Agents; D010879:Piperazines; D010972:Platelet Activating Factor