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[新型磷脂——人类免疫缺陷病毒复制抑制剂。合成与抗病毒活性]

[New phospholipids--inhibitors of human immunodeficiency virus reproduction. Synthesis and antiviral activity].

作者信息

Vodovozova E L, Pavlova Iu B, Polushkina M A, Rzhaninova A A, Garaev M M, Molotkovskiĭ Iu G

出版信息

Bioorg Khim. 1996 Jun;22(6):451-7.

PMID:8975673
Abstract

Several novel phosphatidic acid derivatives of 3'-azido-3'-deoxythymidine and 2',3'-dideoxyinosine were synthesized, which contained dialkylphosphatidyl, dialkylthiophosphatidyl moieties, as well as diacylphosphatidyl moiety with either 14,14,14-trifluoro-12-oxatetradecanoyl or natural acyl residues inherent in egg yolk phosphatidylcholine. Diacylphosphatidyl derivatives of glycyrrhetinic acid were also prepared. All the synthesized compounds exhibited significant anti-HIV activity. The glycyrrhetinic acid derivatives are of special interest because of their low toxicity and a supposedly different mechanism of action.

摘要

合成了几种新型的3'-叠氮基-3'-脱氧胸苷和2',3'-二脱氧肌苷的磷脂酸衍生物,它们含有二烷基磷脂酰、二烷基硫代磷脂酰部分,以及带有14,14,14-三氟-12-氧代十四烷酰基或蛋黄磷脂酰胆碱中固有的天然酰基残基的二酰基磷脂酰部分。还制备了甘草次酸的二酰基磷脂酰衍生物。所有合成的化合物均表现出显著的抗HIV活性。甘草次酸衍生物因其低毒性和推测不同的作用机制而特别受关注。

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