Parallel synthesis of 5-cyano-6-aryl-2-thiouracil derivatives as inhibitors for hepatitis C viral NS5B RNA-dependent RNA polymerase

Through the parallel synthetic strategy, 5-cyano-6-aryl-2-thiouracilderivatives with single digital micromolar inhibitory activity for the hepatitis C viral NS5B RNA-dependent RNA polymerase were obtained. From random screening of our compound libraries, we identified a hit compound with an IC 50 of...

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Veröffentlicht in:Bioorganic chemistry 2006-02, Vol.34 (1), p.26-38
Hauptverfasser: Ding, Yili, Girardet, Jean-Luc, Smith, Kenneth L., Larson, Gary, Prigaro, Brett, Wu, Jim Z., Yao, Nanhua
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Sprache:eng
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Zusammenfassung:Through the parallel synthetic strategy, 5-cyano-6-aryl-2-thiouracilderivatives with single digital micromolar inhibitory activity for the hepatitis C viral NS5B RNA-dependent RNA polymerase were obtained. From random screening of our compound libraries, we identified a hit compound with an IC 50 of 27 μM against hepatitis C viral NS5B RNA-dependent RNA polymerase. By using a parallel synthetic strategy, a series of its derivatives were synthesized. From their anti-HCV activity screening, compounds with single digital 3.8 micromolar activity were obtained.
ISSN:0045-2068
1090-2120
DOI:10.1016/j.bioorg.2005.10.001