Kolocouris N, Foscolos G B, Kolocouris A, Marakos P, Pouli N, Fytas G, Ikeda S, De Clercq E
Department of Pharmacy, University of Athens, Greece.
J Med Chem. 1994 Sep 2;37(18):2896-902. doi: 10.1021/jm00044a010.
The synthesis of some spiro[cyclopropane-1,2'-adamantan]-2-amines and methanamines and some spiro[pyrrolidine-2,2'-adamantanes] is described. The title compounds were evaluated against a wide range of viruses (influenza A, influenza B, parainfluenza 3, RSV, HSV-1, TK- HSV-1, HSV-2, vaccinia, vesicular stomatitis, polio 1, coxsackie B4, sindbis, semliki forest, Reo 1, HIV-1, and HIV-2), and some of them (compounds 6b, 6c, 9a, 16a, 16b, and 17) inhibited the cytopathicity of influenza A virus at a concentration significantly lower than that of amantadine and also significantly lower than the concentrations at which they proved cytotoxic to the host cells. None of the new aminoadamantane derivatives was active against influenza B virus or any of the other viruses tested, which points to their specificity as anti-influenza A virus agents.
描述了一些螺[环丙烷 - 1,2'-金刚烷]-2 - 胺和甲胺以及一些螺[吡咯烷 - 2,2'-金刚烷]的合成。对标题化合物针对多种病毒（甲型流感病毒、乙型流感病毒、副流感病毒3型、呼吸道合胞病毒、单纯疱疹病毒1型、胸苷激酶缺陷型单纯疱疹病毒1型、单纯疱疹病毒2型、痘苗病毒、水疱性口炎病毒、脊髓灰质炎病毒1型、柯萨奇病毒B4、辛德毕斯病毒、Semliki森林病毒、呼肠孤病毒1型、人类免疫缺陷病毒1型和人类免疫缺陷病毒2型）进行了评估，其中一些化合物（化合物6b、6c、9a、16a、16b和17）在显著低于金刚烷胺的浓度下抑制甲型流感病毒的细胞病变效应，并且也显著低于它们对宿主细胞显示细胞毒性的浓度。新的氨基金刚烷衍生物对乙型流感病毒或所测试的任何其他病毒均无活性，这表明它们作为抗甲型流感病毒剂具有特异性。
