Antiviral activity of 2,3′-anhydro and related pyrimidine nucleosides against hepatitis B virus

被引：4

作者：

Srivastav, Naveen C. ^{[1
]}

Mak, Michelle ^{[1
]}

Agrawal, Babita ^{[2
]}

Tyrrell, D. Lorne J. ^{[3
]}

Kumar, Rakesh ^{[1
]}

机构：

[1] Univ Alberta, Dept Lab Med & Pathol, Edmonton, AB T6G 2H7, Canada

[2] Univ Alberta, Dept Surg, Edmonton, AB T6G 2H7, Canada

[3] Univ Alberta, Dept Med Microbiol & Immunol, Fac Med & Dent, Edmonton, AB T6G 2H7, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 22期

基金：

加拿大健康研究院;

关键词：

Hepatitis B virus; Pyrimidine nucleosides; CLOSED CIRCULAR DNA; HEPATOCYTE CULTURES; WILD-TYPE; INHIBITION; LIVER; TRIPHOSPHATES; REPLICATION; POLYMERASE; PREVENTION; INFECTION;

D O I：

10.1016/j.bmcl.2010.08.120

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Various 2,3'-anhydro analogs of 5-substituted 1-(2-deoxy-beta-D-lyxofuranosyl)uracils (10-15) and a related 1-(3-O-mesyl-2-deoxy-beta-D-lyxofuranosyl) pyrimidine nucleoside analog (18) have been synthesized for evaluation as a new class of potential anti-HBV agents. The compounds 10, 12, and 15 demonstrated most potent anti-HBV activities against duck HBV (DHBV) and human HBV with EC50 values in the range of 2.5-10 and 5-10 mu g/mL, respectively, at non-toxic concentrations (CC50 = >200 mu g/mL). The nucleoside 18 also demonstrated significant anti-HBV activity against DHBV with an EC50 value of 2.5 mu g/mL, however, it was less active against HBV in 2.2.15 cells (EC50 = >10 mu g/mL). (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：6790 / 6793

页数：4

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