2,6-Bis-arylmethyloxy-5-hydroxychromones with antiviral activity against both hepatitis C virus (HCV) and SARS-associated coronavirus (SCV)

Title
2,6-Bis-arylmethyloxy-5-hydroxychromones with antiviral activity against both hepatitis C virus (HCV) and SARS-associated coronavirus (SCV)
Authors
김미경유미선박혜리김경보이채운조서영강지훈윤현준김동은추현아정용주정유훈
Keywords
Aryl diketoacid (ADK); 5-Hydroxyflavone; Hepatitis C; Severe Acute Respiratory Syndrome (SARS)
Issue Date
2011-10
Publisher
European journal of medicinal chemistry
Citation
VOL 46, NO 11, 5698-5704
Abstract
In this study, as a bioisosteric alternative scaffold of the antiviral aryl diketoacids (ADKs), we used 5- hydroxychromone on which two arylmethyloxy substituents were installed. The 5-hydroxychromones (5b-5g) thus prepared showed anti-HCV activity and, depending on the aromatic substituents on the 2-arylmethyloxy moiety, some of the derivatives (5b-5f) were also active against SCV. In addition, unlike the ADKs which showed selective inhibition against the helicase activity of the SCV NTPase/helicase, the 5-hydroxychromones (5b-5f) were active against both NTPase and helicase activities of the target enzyme. Among those, 3-iodobenzyloxy-substituted derivative 5e showed the most potent activity against HCV (EC50 = 4 μM) as well as SCV (IC50 = 4 μM for ATPase activity, 11 mM for helicase activity) and this might be used as a platform structure for future development of the multi-target or broad-spectrum antivirals.
URI
http://pubs.kist.re.kr/handle/201004/40503
ISSN
0223-5234
Appears in Collections:
KIST Publication > Article
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