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Synthesis of pyrido-annelated seven-membered N-containing heterocycles

Koen Muylaert (UGent) , Martyna Jatczak (UGent) , Sven Mangelinckx (UGent) and Christian Stevens (UGent)
(2015) CURRENT MEDICINAL CHEMISTRY. 22(9). p.1086-1125
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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
3-]azepines, pyrido[3, pyrido[2, nitrogen heterocycles, Fused-ring system, 4-]azepines, ring construction, synthesis design, INVERSE-ELECTRON-DEMAND, DIELS-ALDER REACTIONS, CHIRAL NADH MODELS, PRIVILEGED STRUCTURES, ANNULATED PYRIDINES, COMBINATORIAL LIBRARIES, DRUG DISCOVERY, ANALOGS, DERIVATIVES, RING

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Citation

Please use this url to cite or link to this publication:

MLA
Muylaert, Koen, et al. “Synthesis of Pyrido-Annelated Seven-Membered N-Containing Heterocycles.” CURRENT MEDICINAL CHEMISTRY, vol. 22, no. 9, 2015, pp. 1086–125.
APA
Muylaert, K., Jatczak, M., Mangelinckx, S., & Stevens, C. (2015). Synthesis of pyrido-annelated seven-membered N-containing heterocycles. CURRENT MEDICINAL CHEMISTRY, 22(9), 1086–1125.
Chicago author-date
Muylaert, Koen, Martyna Jatczak, Sven Mangelinckx, and Christian Stevens. 2015. “Synthesis of Pyrido-Annelated Seven-Membered N-Containing Heterocycles.” CURRENT MEDICINAL CHEMISTRY 22 (9): 1086–1125.
Chicago author-date (all authors)
Muylaert, Koen, Martyna Jatczak, Sven Mangelinckx, and Christian Stevens. 2015. “Synthesis of Pyrido-Annelated Seven-Membered N-Containing Heterocycles.” CURRENT MEDICINAL CHEMISTRY 22 (9): 1086–1125.
Vancouver
1.
Muylaert K, Jatczak M, Mangelinckx S, Stevens C. Synthesis of pyrido-annelated seven-membered N-containing heterocycles. CURRENT MEDICINAL CHEMISTRY. 2015;22(9):1086–125.
IEEE
[1]
K. Muylaert, M. Jatczak, S. Mangelinckx, and C. Stevens, “Synthesis of pyrido-annelated seven-membered N-containing heterocycles,” CURRENT MEDICINAL CHEMISTRY, vol. 22, no. 9, pp. 1086–1125, 2015.
@article{6854974,
  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.}},
  author       = {{Muylaert, Koen and Jatczak, Martyna and Mangelinckx, Sven and Stevens, Christian}},
  issn         = {{0929-8673}},
  journal      = {{CURRENT MEDICINAL CHEMISTRY}},
  keywords     = {{3-]azepines,pyrido[3,pyrido[2,nitrogen heterocycles,Fused-ring system,4-]azepines,ring construction,synthesis design,INVERSE-ELECTRON-DEMAND,DIELS-ALDER REACTIONS,CHIRAL NADH MODELS,PRIVILEGED STRUCTURES,ANNULATED PYRIDINES,COMBINATORIAL LIBRARIES,DRUG DISCOVERY,ANALOGS,DERIVATIVES,RING}},
  language     = {{eng}},
  number       = {{9}},
  pages        = {{1086--1125}},
  title        = {{Synthesis of pyrido-annelated seven-membered N-containing heterocycles}},
  volume       = {{22}},
  year         = {{2015}},
}

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