1,4-Dioxolane-triazaspirodecanone derivatives as nociceptin/orphanin FQ receptor ligands
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- 作者：Sandra Corrado (1)
Claudia Sorbi (1)
Annalisa Tait (1)
Umberto M. Battisti (1)
Valeria Camarda (2)
Davide Malfacini (2)
Girolamo Cal貌 (2)
Livio Brasili (1) - 关键词：NOP receptors ; Spiroxatrine derivatives ; Triazaspirodecanones
- 刊名：Medicinal Chemistry Research
- 出版年：2014
- 出版时间：November 2014
- 年：2014
- 卷：23
- 期：11
- 页码：4642-4656
- 全文大小：989 KB
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Claudia Sorbi (1)
Annalisa Tait (1)
Umberto M. Battisti (1)
Valeria Camarda (2)
Davide Malfacini (2)
Girolamo Cal貌 (2)
Livio Brasili (1)
1. Department of Life Sciences, University of Modena and Reggio Emilia, Via G. Campi 183, 41125, Modena, Italy
2. Department of Medical Sciences, Section of Pharmacology and National Institute of Neuroscience, University of Ferrara, 44121, Ferrara, Italy - ISSN：1554-8120
文摘
A series of N-substituted analogs based upon the spiropiperidine core of the lead compound Spiroxatrine was synthesized. In particular, the new compounds were obtained by replacing the benzodioxane moiety of the Spiroxatrine with several 2-substituted 1,3-dioxolanes. Thus the designed derivatives were synthesized and evaluated as possible NOP receptor ligands. As a conclusion of these studies, the new triazaspirodecanone derivatives showed unique and significant SAR as NOP receptor agonists. In particular, the present study demonstrated that 1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one portion together with appropriate 1,3-dioxolane substituents could lead to a new promising class of NOP receptor ligands.