2',3'-脱水及相关嘧啶核苷对乙型肝炎病毒的抗病毒活性。
Antiviral activity of 2,3'-anhydro and related pyrimidine nucleosides against hepatitis B virus.
机构信息
Department of Laboratory Medicine and Pathology, 1-71 Medical Sciences Building, University of Alberta, Edmonton, AB, Canada T6G 2H7.
出版信息
Bioorg Med Chem Lett. 2010 Nov 15;20(22):6790-3. doi: 10.1016/j.bmcl.2010.08.120. Epub 2010 Sep 20.
Various 2,3'-anhydro analogs of 5-substituted 1-(2-deoxy-β-d-lyxofuranosyl)uracils (10-15) and a related 1-(3-O-mesyl-2-deoxy-β-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 EC(50) values in the range of 2.5-10 and 5-10 μg/mL, respectively, at non-toxic concentrations (CC(50) = > 200 μg/mL). The nucleoside 18 also demonstrated significant anti-HBV activity against DHBV with an EC(50) value of 2.5 μg/mL, however, it was less active against HBV in 2.2.15 cells (EC(50) = > 10 μg/mL).
已经合成了各种 5-取代的 1-(2-脱氧-β-d-乳呋喃基)尿嘧啶核苷（10-15）和相关的 1-(3-O-甲磺酰基-2-脱氧-β-d-乳呋喃基)嘧啶核苷类似物（18）的 2,3'-脱水类似物，以评估它们作为一类新的潜在抗乙型肝炎病毒（HBV）药物的潜力。化合物 10、12 和 15 在非毒性浓度下（CC50>200μg/mL）对鸭乙型肝炎病毒（DHBV）和人乙型肝炎病毒（HBV）表现出最强的抗 HBV 活性，EC50 值分别在 2.5-10 和 5-10μg/mL 范围内。核苷 18 对 DHBV 也表现出显著的抗 HBV 活性，EC50 值为 2.5μg/mL，但在 2.2.15 细胞中对 HBV 的活性较低（EC50>10μg/mL）。
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