Department of Bioscience and Biotechnology, Bio/Molecular Informatics Center, Konkuk University, Seoul 143-701, Korea.
Arch Pharm Res. 2012 Jan;35(1):77-85. doi: 10.1007/s12272-012-0108-9. Epub 2012 Feb 2.
Aryl diketoacid (ADK) is well known for antiviral activity which can be enhanced by introduction of an aromatic arylmethyl substituent. A natural flavonoid quercetin has a 3,5-dihydroxychromone pharmacophore which is in bioisosteric relationship with the 1,3-diketoacid moiety of the ADK. Thus, it was of our interest to test the antiviral activity of the quercetin derivatives with an arylmethyl group attached. In this study, we prepared a series of the 7-O-arylmethylquercetin derivatives with various aromatic substituents and evaluated their antiviral activity against the SARS-associated coronavirus (SARS-CoV, SCV) as well as hepatitis C virus (HCV). Single difference in the aromatic substituent fine-tuned the biological activity of the 7-O-arylmethylquercetin derivatives to result in two different classes of derivatives selectively active against SCV and HCV.
芳基二酮酸（ADK）具有抗病毒活性，通过引入芳香芳基甲基取代基可以增强其活性。天然类黄酮槲皮素具有 3,5-二羟基色酮药效团，与 ADK 的 1,3-二酮酸部分具有生物等排关系。因此，我们有兴趣测试具有芳基甲基的槲皮素衍生物的抗病毒活性。在这项研究中，我们制备了一系列带有各种芳香取代基的 7-O-芳基甲基槲皮素衍生物，并评估了它们对 SARS 相关冠状病毒（SARS-CoV，SCV）和丙型肝炎病毒（HCV）的抗病毒活性。芳香取代基的单一差异微调了 7-O-芳基甲基槲皮素衍生物的生物活性，导致针对 SCV 和 HCV 具有两种不同活性类别的衍生物。
