- 4′-Modified Pyrimidine Nucleosides as Potential Anti-hepatitis C Virus (HCV) Agents
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Herein, we have investigated novel pyrimidine nucleosides bearing a 4'-carboxyl functionality (6-10, 13 and 15) as anti-HCV agents. In this new class of compounds, 7, 9, 10 and 15 demonstrated in vitro anti-HCV activity similar to or better than a known anti-HCV drug, ribavirin. In this work, we also, surprisingly, identified a 3'-sulfoxide analog of 3′-thiacytidine (16), obtained as a side product during the synthesis of 15, as a potent inhibitor of HCV replication at the concentration similar to that of ribavirin. No detectable in vitro cytotoxicity was observed for the investigated compounds up to the highest concentration tested.
- Shakya, Neeraj,Vedi, Satish,Liang, Chao,Agrawal, Babita,Kumar, Rakesh
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p. 917 - 921
(2014/07/21)
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- PROCESS FOR PREPARATION OF CIS-NUCLEOSIDE DERIVATIVE
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The present invention relates to a novel and stereoselective synthetic process for the preparation of optically active cis-nucleoside derivatives of compound of Formula (I), wherein R3 represents H, F, Cl, C1-16 alkyl.
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Page/Page column 12
(2011/11/30)
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- PROCESS FOR THE PREPARATION OF CIS-NUCLEOSIDE DERIVATIVE
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The present invention relates to a novel and stereoselective synthetic process for the preparation of optically active cis-nucleoside derivatives of compound of Formula (I), wherein R3 represents H, F, Cl, C1-16 alkyl.
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Page/Page column 32
(2010/08/08)
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- 2-Substituted-4-substituted-1,3-dioxolanes and use thereof
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Nucleoside analogues containing a 1,3-dioxolane structure are suitable antiviral agents, particulary for the treatment of the HIV infections in mammals, especially humans. Examples of the nucleoside analogues include: cis-2-acetoxymethyl-4-(thymin-1′-yl)-1,3,-dioxolane, cis-2-hydroxymethyl-4-(thymin-1′-yl)-1,3-dioxolane, cis-2-benzoyloxymethyl-4-(cytosin-1′-yl)-1,3-dioxolane, and cis-2-hydroxymethyl-4-(cytosin-1′-yl)-1,3-dioxolane. These compounds can be in the form of their racemates or their separate enantiomers.
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Page column 40
(2010/11/29)
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