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KMID : 0043320120350010077
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Archives of Pharmacal Research
2012 Volume.35 No. 1 p.77 ~ p.85
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Synthesis and antiviral evaluation of 7-O-arylmethylquercetin derivatives against SARS-associated coronavirus (SCV) and hepatitis C virus (HCV)
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Park Hye-Ri
Yoon Hyun-Jun
Kim Mi-Kyoung
Lee Sung-Dae
Chong You-Hoon
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Abstract
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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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KEYWORD
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Quercetin, Arylmethyl, Hepatitis C, Severe acute respiratory syndrome (SARS)
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