Synthesis and antiviral evaluation of 7-<Emphasis Type="Italic">O</Emphasis>-arylmethylquercetin derivatives against SARS-associated coronavirus (SCV) and hepatitis C virus (HCV) |
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Authors: | Hye Ri Park Hyunjun Yoon Mi Kyoung Kim Sung Dae Lee Youhoon Chong |
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Institution: | Department of Bioscience and Biotechnology, Bio/Molecular Informatics Center, Konkuk University, Seoul 143-701, Korea. |
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Abstract: | 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. |
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