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一种新型金刚烷化合物的体外抗病毒活性及初步临床试验

In vitro antiviral activity and preliminary clinical trials of a new adamantane compound.

作者信息

Mathur A, Beare A S, Reed S E

出版信息

Antimicrob Agents Chemother. 1973 Oct;4(4):421-6. doi: 10.1128/AAC.4.4.421.

Abstract

A compound, 1'-methyl spiro (adamantane-2,3'-pyrrolidine) maleate, chemically related to the antiviral drug amantadine, was tested for activity in vitro against a number of human respiratory viruses. By a variety of techniques, it was shown to be active against a wide range of human and animal influenza A viruses. The effect was, however, variable and ranged from high activity against two 1957 Asian strains to no observable activity against a 1971 strain. Like amantadine, the drug did not inhibit the growth of influenza B viruses. It was also inactive against a number of paramyxoviruses. Unlike amantadine, the drug did inhibit rhinoviruses, but to a lesser extent than myxoviruses. The coronavirus 229E was also sensitive to the action of the drug in vitro. Although an earlier trial in volunteers showed that, when given orally from 2 days before until 5 days after virus challenge, the drug was protective against infection with influenza A/Hong Kong/68 virus, a similar trial in volunteers challenged with rhinoviruses 2 and 9 revealed no useful activity against rhinoviruses in man.

摘要

一种与抗病毒药物金刚烷胺化学相关的化合物——马来酸1'-甲基螺(金刚烷-2,3'-吡咯烷),针对多种人类呼吸道病毒进行了体外活性测试。通过多种技术表明,它对多种人类和动物甲型流感病毒具有活性。然而,其效果存在差异,从对两种1957年亚洲毒株的高活性到对1971年一种毒株无明显活性不等。与金刚烷胺一样,该药物不抑制乙型流感病毒的生长。它对多种副粘病毒也无活性。与金刚烷胺不同的是,该药物确实能抑制鼻病毒,但程度低于粘液病毒。冠状病毒229E在体外对该药物的作用也敏感。尽管早期在志愿者中进行的一项试验表明,在病毒攻击前2天至攻击后5天口服该药物,可预防甲型流感病毒/香港/68感染,但在感染鼻病毒2型和9型的志愿者中进行的类似试验显示,该药物对人类鼻病毒无有效活性。

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