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[金刚乙胺的3-取代类似物:在Vero细胞中的合成及抗疱疹活性]

[3-substituted analogs of remantadine: synthesis and antiherpetic activity in Vero cells].

作者信息

Moiseev I K, Andronova V L, Pozdniakov V V, Makarova N V, Galegov G A

机构信息

D. I. Ivanovsky Research Institure of Virology Russian Academy of Medical Sciences, Moscow.

出版信息

Antibiot Khimioter. 2002;47(11):9-12.

PMID:12698574
Abstract

Chemical synthesis of 3-substituted analogues of remantadine is described. Derivatives IIIb and IIIc when compared with remantadine had not only potent activity against ethalon herpes simplex type 1 virus strain but also were active against herpes virus resistant to aciclovir. Compound IIIc demonstrated virulecidal effect. Combination of IIIc + aciclovir had additive effect against ethalon herpes simplex type 1 virus strain. Investigated 3-substituted analogues demonstrated low activity in the model system of influenzae virus. No antiviral activity was demonstrated in the model system of Syndbys virus (though compounds were evaluated in subtoxic concentrations).

摘要

描述了金刚乙胺3-取代类似物的化学合成。与金刚乙胺相比,衍生物IIIb和IIIc不仅对埃塔龙单纯疱疹病毒1型毒株具有强效活性,而且对阿昔洛韦耐药的疱疹病毒也有活性。化合物IIIc表现出杀病毒作用。IIIc +阿昔洛韦组合对埃塔龙单纯疱疹病毒1型毒株具有相加作用。所研究的3-取代类似物在流感病毒模型系统中表现出低活性。在辛德毕斯病毒模型系统中未显示抗病毒活性(尽管化合物是以亚毒性浓度进行评估的)。

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