摘要
医药行业中受到缺乏的潜在药物的困惑。然而,仍有个很好的机会为药物化学精心设计有趣的骨架。各种具有潜力的骨架在文献中没有(或很少)被研究或没有(或只有几次)被描述。在过去的几十年中,广泛的苯二氮卓类衍生物的生物活性进行了深入的研究并取得了一些药物骨架,尤其是1,4 -苯二氮卓类系列。它是药物发现中最重要的结构之一。对苯二氮卓类实质研究引导具有潜在的、新药理活性的氮杂衍生物合成。已知一些吡啶并吖庚因类在中枢神经系统具有很强的活性,其活性甚至可以和著名的苯二氮卓类骨架相提并论,这为吡啶并吖庚因类研究和合成提供了一个重要的研究主题。
关键词: 稠环系统,含氮杂环化合物,吡啶并[2,3 ]氮杂卓,吡啶并[3,4 ]氮杂卓,环结构,设计合成。
Current Medicinal Chemistry
Title:Synthesis of Pyrido-Annelated Seven-Membered N-Containing Heterocycles
Volume: 22 Issue: 9
Author(s): Koen Muylaert, Martyna Jatczak, Sven Mangelinckx and Christian V. Stevens
Affiliation:
关键词: 稠环系统,含氮杂环化合物,吡啶并[2,3 ]氮杂卓,吡啶并[3,4 ]氮杂卓,环结构,设计合成。
摘要: The pharmaceutical industry is struggling with a lack of potential drugs in the pipe line. However, there is still a great opportunity to elaborate interesting scaffolds for medicinal chemistry. Various scaffolds that hold promise are not (or little) studied or are not (or only a few times) described in literature. For the last couple of decades, a wide range of biological activities of benzodiazepine derivatives have been investigated thoroughly and have made the benzodiazepine scaffold, particularly the 1,4-benzodiazepine system, one of the most important structures for drug discovery. The substantial research on benzodiazepines has led to the synthesis of heterocycle-fused azepine derivatives with potentially new pharmacological activity. Some pyridoazepines are known to be active in the central nervous system and have a comparable activity to the well-known benzodiazepine scaffolds, which make the synthesis and the study of pyridoazepines an important research topic.
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Cite this article as:
Koen Muylaert, Martyna Jatczak, Sven Mangelinckx and Christian V. Stevens , Synthesis of Pyrido-Annelated Seven-Membered N-Containing Heterocycles, Current Medicinal Chemistry 2015; 22 (9) . https://dx.doi.org/10.2174/0929867322666141212114856
DOI https://dx.doi.org/10.2174/0929867322666141212114856 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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