- Discovery of a 2′-fluoro-2′-C-methyl C-nucleotide HCV polymerase inhibitor and a phosphoramidate prodrug with favorable properties
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A series of 2′-fluorinated C-nucleosides were prepared and tested for anti-HCV activity. Among them, the triphosphate of 2′-fluoro-2′-C-methyl adenosine C-nucleoside (15) was a potent and selective inhibitor of the NS5B polymerase and maintained activity
- Kirschberg, Thorsten A.,Metobo, Sammy,Clarke, Michael O.,Aktoudianakis, Vangelis,Babusis, Darius,Barauskas, Ona,Birkus, Gabriel,Butler, Thomas,Byun, Daniel,Chin, Gregory,Doerffler, Edward,Edwards, Thomas E.,Fenaux, Martijn,Lee, Rick,Lew, Willard,Mish, Michael R.,Murakami, Eisuke,Park, Yeojin,Squires, Neil H.,Tirunagari, Neeraj,Wang, Ting,Whitcomb, Mark,Xu, Jie,Yang, Huiling,Ye, Hong,Zhang, Lijun,Appleby, Todd C.,Feng, Joy Y.,Ray, Adrian S.,Cho, Aesop,Kim, Choung U.
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p. 1840 - 1847
(2017/04/04)
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- 2'-FLUORO SUBSTITUTED CARBA-NUCLEOSIDE ANALOGS FOR ANTIVIRAL TREATMENT
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Provided are pyrrolo[1,2-f][1,2,4]triazinyl, imidazo[1,5-f][1,2,4]triazinyl, imidazo[1,2-f][1,2,4]triazinyl, and [1,2,4]triazolo[4,3-f][1,2,4]triazinyl nucleosides, nucleoside phosphates and prodrugs thereof, wherein the 2′ position of the nucleoside suga
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