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Structure-activity relationships in platelet-activating factor. 12. Synthesis and biological evaluation of platelet-activating factor antagonists with anti-HIV-1 activity.

Abstract：

:The HIV-1 central nervous system infection leads to the onset of neurological impairments called AIDS dementia complex (ADC). PAF plays an important role in this pathology, as it is an HIV-1-induced neurotoxin produced by infected or activated macrophages and microglia, in the brain. We previously reported that PAF-antagonists bearing a trisubstituted piperazine presented in vitro anti-HIV-1 activity in human macrophages. To improve the pharmacological activities of our lead compound, 1a, we modified its carbamate function and evaluated both its antiretroviral and anti-PAF activities. One carbamate derivative (10c) demonstrated a similar antiviral activity but a higher anti-PAF potency, whereas 4a, with an ureide function, presents an increased antiviral activity and can be considered as a pure antiretroviral drug, as it does not present PAF-antagonism. Moreover, we measured the ability of 1a to cross the blood-brain barrier, using the in situ mouse brain perfusion method and its plasmatic concentrations after iv and po administration. The transport parameter measured (K(in)) proves that 1a is able to cross this biological barrier, but a pharmacokinetic study reveals its weak bioavailability in rats.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Serradji N,Martin M,Bensaid O,Cisternino S,Rousselle C,Dereuddre-Bosquet N,Huet J,Redeuilh C,Lamouri A,Dong CZ,Clayette P,Scherrmann JM,Dormont D,Heymans F

doi

10.1021/jm040860g

keywords:

subject

Has Abstract

pub_date

2004-12-02 00:00:00

pages

6410-9

issue

25

eissn

0022-2623

issn

1520-4804

journal_volume

47

pub_type

杂志文章

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