کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1369475 | 981779 | 2012 | 6 صفحه PDF | دانلود رایگان |

Hepatitis B virus (HBV) and hepatitis C virus (HCV) infections are major health threats worldwide leading to liver cirrhosis, liver cancer and mortality. Herein, we report a new category of dideoxy pyrimidine nucleosides possessing a 4′-carboxyl (or carboxymethyl) function (7–9, 13, 16, 17), which are discovered as potential antiviral agents. For the first time, these nucleosides are recognized to be inhibitors of HBV and/or HCV replication. Among 4′-carboxy compounds, 3′,4′-didehydrothymidine (16) was most effective against DHBV, HBV and HCV. Modification of the 4′-position in compound 7 from a carboxyl to carboxymethyl group (17) did not affect the anti-HBV activity but greatly increased the anti-HCV activity. Importantly, 17 yielded synergistic antiviral effect when combined with ribavirin without toxicity. The activity exhibited by a single agent towards both hepatitis viruses and no detectable in vitro cytotoxicity make this new class of compounds of interest.
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Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 20, 15 October 2012, Pages 6475–6480