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 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.
Van Derpoorten
K
K
Ecole de Pharmacie, Faculté de Médecine, Université Catholique de Louvain, Bruselles, Belgium.
Balzarini
J
J
De Clercq
E
E
Poupaert
J H
JH
D000218:Adamantane / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D019380:Anti-HIV Agents / Q000737:chemistry / Q000494:pharmacology*; D001549:Benzamides / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D015498:HIV-2 / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D010672:Phenytoin / Q000737:chemistry / Q000494:pharmacology; D010797:Phthalimides / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013601:T-Lymphocytes; D013792:Thalidomide / Q000031:analogs & derivatives; D014779:Virus Replication / Q000187:drug effects*
D019380:Anti-HIV Agents; D001549:Benzamides; C116325:N-1-adamantyl-4-aminophthalimide; D010797:Phthalimides; D013792:Thalidomide; D010672:Phenytoin; C055323:ameltolide; D000218:Adamantane