کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1369475 981779 2012 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
A new class of pyrimidine nucleosides: inhibitors of hepatitis B and C viruses
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
A new class of pyrimidine nucleosides: inhibitors of hepatitis B and C viruses
چکیده انگلیسی

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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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 20, 15 October 2012, Pages 6475–6480
نویسندگان
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