[无机焦磷酸盐的非水解类似物作为丙型肝炎病毒rna依赖rna聚合酶抑制剂]。

Bioorganicheskaia khimiia Pub Date : 2012-03-01
D V Ianvarev, A N Korovina, N N Usanov, S N Kochetkov
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引用次数: 0

摘要

无机焦磷酸盐(PPi)是由DNA聚合酶和rna聚合酶催化的聚合反应产物。我们已经合成了一些新的不可水解的PPi类似物,其中一些已经被证明对丙型肝炎病毒rna依赖rna聚合酶(NS5B)催化的聚合反应有抑制作用。以非水解二膦酸亚甲酯为骨架,开发了一种新的药效团。对12种双膦酸盐进行了构效关系分析,确定了其抑制NS5B聚合酶活性的关键结构特征。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
[Non-hydrolysable analogs of inorganic pyrophosphate as inhibitors of hepatitis C virus RNA-dependent RNA-polymerase].

Inorganic pyrophosphate (PPi) is a product of the polymerization reaction catalyzed by DNA- and RNA-polymerases. We have synthesized a number of novel non-hydrolysable PPi analogues, some of them have demonstrated inhibition of polymerization reaction catalyzed by hepatitis C virus RNA-dependent RNA-polymerase (NS5B). A new pharmacophore has been developed based on non-hydrolysable methylene-diphosphonate backbone. Structure-activity relationship analysis of 12 bisphosphonates is presented and structural features crucial for the ability of molecule to inhibit NS5B polymerase activity are ascertained.

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