Structure-activity relationship studies on anti-HCV activity of ring-expanded ('fat') nucleobase analogues containing the imidazo[4,5-e][1,3]diazepine-4,8-dione ring system.
Structure-activity relationship studies on anti-HCV activity of ring-expanded ('fat') nucleobase analogues containing the imidazo[4,5-e][1,3]diazepine-4,8-dione ring system.
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DOI：
10.1016/j.bmcl.2007.01.085
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发表时间：
2007-04
影响因子：
2.7
通讯作者：
Peng Zhang;Ning Zhang;B. Korba;R. Hosmane
中科院分区：
文献类型：
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作者：
Peng Zhang;Ning Zhang;B. Korba;R. Hosmane
在我们对咪唑并[4，5-e][1，3]二氮杂环体系抗丙型肝炎病毒活性的构效关系研究的基础上，我们报道了杂环2-位引入疏水取代基的合成及其对生物活性的影响。我们的结果表明，在这方面没有特别的优势，因为观察到的测试化合物的抗病毒活性低于用于比较的未经修饰的2-溴衍生物。然而，所有目标化合物的活性/毒性分布仍然好于抗病毒检测中使用的参比化合物利巴韦林，但不如检测中使用的另一种参比化合物干扰素-α。
In continuation of our structure–activity relationship studies on anti-HCV activity of the title imidazo[4,5-e][1,3]diazepine ring system, we report here the synthesis and effect on biological activity of introducing hydrophobic substituents at the 2-position of the heterocycle. Our results suggest that there is no particular advantage to that end as the observed antiviral activity of the test compounds was lower than that of the unmodified 2-bromo derivative used for comparison. The activity/toxicity profile of all target compounds, however, was still better than that of the reference compound ribavirin used in the antiviral assay, but not as good as that of interferon-α, the other reference compound used in the assay.