Abstract
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.
Keywords: Hepatitis C virus, Anti-HCV effect, Synthesis, Nucleosides.
Letters in Drug Design & Discovery
Title:4'-Modified Pyrimidine Nucleosides as Potential Anti-hepatitis C Virus (HCV) Agents
Volume: 11 Issue: 7
Author(s): Neeraj Shakya, Satish Vedi, Chao Liang, Babita Agrawal and Rakesh Kumar
Affiliation:
Keywords: Hepatitis C virus, Anti-HCV effect, Synthesis, Nucleosides.
Abstract: 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.
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Cite this article as:
Shakya Neeraj, Vedi Satish, Liang Chao, Agrawal Babita and Kumar Rakesh, 4'-Modified Pyrimidine Nucleosides as Potential Anti-hepatitis C Virus (HCV) Agents, Letters in Drug Design & Discovery 2014; 11 (7) . https://dx.doi.org/10.2174/1570180811666140401184856
DOI https://dx.doi.org/10.2174/1570180811666140401184856 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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