Anti-HIV activity of N-1-adamantyl-4-aminophthalimide

The discovery of new leads acting via novel modes of action in the treatment of the human immunodeficiency virus (HIV), the causative agent of AIDS, remains a challenge. Along this line we synthesized and evaluated a series of N-substituted 4-aminophthalimides which were designed according to the mo...

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Bibliographic Details
Published in:Biomedicine & pharmacotherapy 1997-01, Vol.51 (10), p.464-468
Main Authors: Van Derpoorten, K, Balzarini, J, De Clercq, E, Poupaert, J.H.
Format: Article
Language:English
Subjects:
Adamantane - analogs & derivatives
Adamantane - chemistry
Adamantane - pharmacology
AIDS
AIDS/HIV
anti-HIV activity
Anti-HIV Agents - chemistry
Anti-HIV Agents - pharmacology
Benzamides - chemistry
Benzamides - pharmacology
Cell Line
Cell Survival - drug effects
HIV-1 - drug effects
HIV-1 - physiology
HIV-2 - drug effects
HIV-2 - physiology
Humans
phenytoin
Phenytoin - chemistry
Phenytoin - pharmacology
phthalimide
Phthalimides - chemistry
Phthalimides - pharmacology
Structure-Activity Relationship
T-Lymphocytes
thalidomide
Thalidomide - analogs & derivatives
Virus Replication - drug effects
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Summary:The discovery of new leads acting via novel modes of action in the treatment of the human immunodeficiency virus (HIV), the causative agent of AIDS, remains a challenge. Along this line we synthesized and evaluated a series of N-substituted 4-aminophthalimides which were designed according to the models of thalidomide, phenytoin (PHT) and ameltolide. From a series of 24 compounds only N-1-adamantyl-4-aminophthalimide was endowed with anti-HIV-1 and -HIV-2 activity in CEM cell cultures.
ISSN:0753-3322
1950-6007
DOI:10.1016/S0753-3322(97)82327-X