“Viologen” Dendrimers as Antiviral Agents: The Effect of Charge Number and Distance
作者:Simona Asaftei、Erik De Clercq
DOI:10.1021/jm100093p
日期:2010.5.13
A series of “viologen” derivatives (4,4′-bipyridinium salts) carrying between 1 and 90 charges per molecule have been prepared and investigated for their activity against human immunodeficiency virus (HIV), herpes simplex virus (HSV), vesicular stomatitis, Punta Toro virus, Sindbis virus, Reovirus, and respiratory syncytial viruses. In general, most of the compounds showed good activities against HIV-1
制备了一系列每个分子带有1至90个电荷的“ viologen”衍生物(4,4'-联吡啶鎓盐),并研究了其对人类免疫缺陷病毒(HIV),单纯疱疹病毒(HSV),水疱性口腔炎,蓬塔托罗病毒,辛德比斯病毒,呼肠孤病毒和呼吸道合胞病毒。通常,大多数化合物对HIV-1(III B株)显示出良好的活性。尤其是,化合物36在MT-4细胞中表现出最高的针对HIV-1(III B株)的体外活性和选择性指数(EC 50 = 0.26±0.08μM,SI = 75.7)。结果暗示抗病毒活性需要最佳数量和距离的正电荷。