Journal of Microbiology and Biotechnology

The Korean Society for Microbiology and Biotechnology (한국미생물·생명공학회)
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Evaluation of Inhibitory Effects of Thiobarbituric Acid Derivatives Targeting HCV NS5B Polymerase

  • Lee, Jong-Ho (Department of Bioscience and Biotechnology, Hankuk University of Foreign Studies) ;
  • Lee, Sang-Yoon (Department of Bioscience and Biotechnology, Hankuk University of Foreign Studies) ;
  • Park, Mi-Young (Department of Bioscience and Biotechnology, Hankuk University of Foreign Studies) ;
  • Ha, Hyun-Joon (Department of Chemistry, Hankuk University of Foreign Studies) ;
  • Myung, Hee-Joon (Department of Bioscience and Biotechnology, Hankuk University of Foreign Studies)
  • Received : 2009.10.16
  • Accepted : 2009.11.04
  • Published : 2010.03.31
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Abstract

A series of thiobarbituric acid derivatives were constructed and evaluated for inhibitory activity on hepatitis C virus NS5B polymerase. In biochemical assays using purified viral polymerase and RNA template, the $IC_{50}$ value was improved to 0.41 ${\mu}M$ from the original compound's 1.7 ${\mu}M$ value. In HCV sub genomic replicon assay, the $EC_{50}$ value was improved to 3.7 ${\mu}M$ from the original compound's 12.3 ${\mu}M$ value. $CC_{50}$ was higher than 77 ${\mu}M$ for all compounds tested, suggesting that they are useful candidates for anti-HCV therapy.

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References

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