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 |
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Hauptverfasser: | , , , , , , |
Format: | Artikel |
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. |
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ISSN: | 0045-2068 1090-2120 |
DOI: | 10.1016/j.bioorg.2005.10.001 |