具有生物学意义的金刚烷衍生物。2-(1-金刚烷基)咪唑衍生物的合成与抗病毒活性。
Adamantane derivatives of biological interest. Synthesis and antiviral activity of 2-(1-adamantyl)imidazole derivatives.
作者信息
Pellicciari R, Fioretti M C, Cogolli P, Tiecco M
出版信息
Arzneimittelforschung. 1980;30(12):2103-5.
The methods of synthesis and antiviral evaluation of 2-(1-adamantyl)imidazole (2a), N-methyl-2-(1-adamantyl)imidazole (2b) and 2-(1-adamantyl)benzimidazole (3a) are reported. These compounds are prepared by the selective homolytic substitution reaction by the adamantyl radical (Ad.) on the C-2 carbon atom of the heterocycles. Ad. radicals were generated by oxidative decarboxylation of 1-adamantyl carboxylic acid. Antiviral activities compounds 2a, 2b and 3a were tested in chick embryos against A-2 Victoria virus. Compounds 2a and 2b showed significant antiviral activity, whereas compound 3a was found inactive.
报道了2-(1-金刚烷基)咪唑(2a)、N-甲基-2-(1-金刚烷基)咪唑(2b)和2-(1-金刚烷基)苯并咪唑(3a)的合成方法及抗病毒评估。这些化合物是通过金刚烷基自由基(Ad.)对杂环C-2碳原子的选择性均裂取代反应制备的。Ad.自由基由1-金刚烷羧酸的氧化脱羧反应产生。化合物2a、2b和3a的抗病毒活性在鸡胚中针对A-2维多利亚病毒进行了测试。化合物2a和2b表现出显著的抗病毒活性，而化合物3a被发现无活性。
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