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.

1,4-Dioxolane-triazaspirodecanone derivatives as nociceptin/orphanin FQ receptor ligands / Corrado, Sandra; Sorbi, Claudia; Tait, Annalisa; Battisti, Umberto M.; Camarda, Valeria; Malfacini, Davide; Calò, Girolamo; Brasili, Livio. - In: MEDICINAL CHEMISTRY RESEARCH. - ISSN 1054-2523. - STAMPA. - 23:11(2014), pp. 4642-4656. [10.1007/s00044-014-1032-y]

1,4-Dioxolane-triazaspirodecanone derivatives as nociceptin/orphanin FQ receptor ligands

SORBI, Claudia;TAIT, Annalisa;BRASILI, Livio
2014

Abstract

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.
23
11
4642
4656
1,4-Dioxolane-triazaspirodecanone derivatives as nociceptin/orphanin FQ receptor ligands / Corrado, Sandra; Sorbi, Claudia; Tait, Annalisa; Battisti, Umberto M.; Camarda, Valeria; Malfacini, Davide; Calò, Girolamo; Brasili, Livio. - In: MEDICINAL CHEMISTRY RESEARCH. - ISSN 1054-2523. - STAMPA. - 23:11(2014), pp. 4642-4656. [10.1007/s00044-014-1032-y]
Corrado, Sandra; Sorbi, Claudia; Tait, Annalisa; Battisti, Umberto M.; Camarda, Valeria; Malfacini, Davide; Calò, Girolamo; Brasili, Livio
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11380/1062702
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