Abstract
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.
Keywords: Fused-ring system, nitrogen heterocycles, pyrido[2, 3-]azepines, pyrido[3, 4-]azepines, ring construction, synthesis design.
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:
Keywords: Fused-ring system, nitrogen heterocycles, pyrido[2, 3-]azepines, pyrido[3, 4-]azepines, ring construction, synthesis design.
Abstract: 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:
Muylaert Koen, Jatczak Martyna, Mangelinckx Sven and Stevens V. Christian, 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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