2,3-Dihydro-1,2-Diphenyl-substituted 4H-Pyridinone Derivatives as New Anti Flaviviridae Inhibitors
作者:Antonella Peduto、Antonio Massa、Antonia Di Mola、Paolo de Caprariis、Paolo La Colla、Roberta Loddo、Sergio Altamura、Giovanni Maga、Rosanna Filosa
DOI:10.1111/j.1747-0285.2011.01102.x
日期:2011.6
With the aim of identifying novel lead compounds active against emergent human infectious diseases, a series of 2,3‐dihydro‐4H‐pyridinone derivatives has been prepared and evaluated for antiviral activity. Compounds were evaluated in vitro in cell‐based assays for cytotoxicity and against a wide spectrum of viruses. In the antiviral screening, several compounds showed to be fairly active against viruses
为了鉴定对人类新兴传染病具有活性的新型先导化合物,已制备了一系列2,3-二氢-4H-吡啶酮衍生物,并对其抗病毒活性进行了评估。在基于细胞的测定法中对化合物进行了体外评估,以评估其细胞毒性和对多种病毒的毒性。在抗病毒筛选中,几种化合物显示出对黄病毒科病毒的相当活性。的瘟病毒属(牛病毒性腹泻病毒)通过抑制4A顺式(CC 50 > 100μ米; EC 50 = 14μ米,化合物)4C顺式和6a中显示针对一个显著活性黄病毒(黄热病毒)(CC 50 > 100μ米; EC 50 = 18μ米,CC 50 > 100μ米; EC 50 = 10μ米)。在这些中,化合物6A中显示很大的抑制活性对丙型肝炎病毒属中复制子测定[CC(丙型肝炎病毒)50 > 100μ米; EC 50(1b)=4μm。体外讨论了对标题化合物的HCV RNA依赖性RNA聚合酶(NS5B)的抑制活性。对病毒株的抗病毒筛选表