Synthesis of N3,5'-cyclo-4-(beta-D-ribofuranosyl)-vic-triazolo[4,5-b]pyridin-5-one and its 3'-deoxysugar analogue as potential anti-hepatitis C virus agents |
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| Authors: | Wang Peiyuan Hollecker Laurent Pankiewicz Krzysztof W Patterson Steven E Whitaker Tony McBrayer Tamara R Tharnish Phillip M Stuyver Lieven J Schinazi Raymond F Otto Michael J Watanabe Kyoichi A |
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| Institution: | Department of Chemistry, Pharmasset, Inc., Tucker, GA 30084, USA. |
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| Abstract: | We recently discovered a novel compound, identified as N3, 5-cyclo-4-(beta-D-ribofuranosyl)-vic-triazolo4,5-b]pyridinin-5-one, with anti-hepatitis C virus (HCV) activity in vitro. The structure was confirmed by chemical synthesis from 2-hydroxy-5-nitropyridine. It showed anti-HCV activity with EC50= 19.7 microM in replicon cells. Its 3'-deoxy sugar analogue was also synthesized, but was inactive against HCV in vitro. |
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