N-1-金刚烷基-4-氨基邻苯二甲酰亚胺的抗HIV活性
Anti-HIV activity of N-1-adamantyl-4-aminophthalimide.
作者信息
Van Derpoorten K, Balzarini J, De Clercq E, Poupaert J H
机构信息
Ecole de Pharmacie, Faculté de Médecine, Université Catholique de Louvain, Bruselles, Belgium.
出版信息
Biomed Pharmacother. 1997;51(10):464-8. doi: 10.1016/s0753-3322(97)82327-x.
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.
在治疗获得性免疫缺陷综合征（AIDS）的病原体——人类免疫缺陷病毒（HIV）方面，通过新型作用模式发挥作用的新先导化合物的发现仍然是一项挑战。沿着这一思路，我们合成并评估了一系列根据沙利度胺、苯妥英（PHT）和美索巴莫的模型设计的N-取代4-氨基邻苯二甲酰亚胺。在CEM细胞培养中，从一系列24种化合物中，只有N-1-金刚烷基-4-氨基邻苯二甲酰亚胺具有抗HIV-1和抗HIV-2活性。
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